Publications - Sophion

Wnts control membrane potential in mammalian cancer cells

Author(s): Jonathan Ashmore, Hervør Olsen, Naja Sørensen, Christopher Thrasivoulou, Aamir Ahmed

Voltage-Gated Ion Channels in Cancer Cell Proliferation

Author(s): Vidhya R. Rao 1 , Mathew Perez-Neut 1, Simon Kaja 2 and Saverio Gentile 1,*

Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel NaV1.1 Provide Novel Leads for Development of Antiepileptic Drugs

Author(s): Chun Yuen Chow, Yanni K.-Y. Chin, Andrew A. Walker, Shaodong Guo, Linda V. Blomster, Micaiah J. Ward, Volker Herzig, Darin R. Rokyta, and Glenn F. King

Venom chemistry underlying the painful stings of velvet ants (Hymenoptera: Mutillidae)

Author(s): Jensen, T., Walker, A. A., Nguyen, S. H., Jin, A.-H., Deuis, J. R., Vetter, I., King, G. F., Schmidt, J. O., & Robinson, S. D.

Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia

Author(s): Damian Bell, Mark Dallas

Use of automated patch clamp in cardiac safety assessment: past, present and future perspectives

Journal: Journal of Pharmcological and Toxicological Methods
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Author(s): Bell, D.C. & Fermini, B.

Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency

Author(s): Alicia Peschel, Fernanda C. Cardoso, Andrew A. Walker, Thomas Durek, M. Rhia L. Stone, Nayara Braga Emidio, Philip E. Dawson, Markus Muttenthaler, and Glenn F. King

Tricyclic Triazoles as σ1Receptor Antagonists for Treating Pain

Author(s): Díaz, J. L., Cuevas, F., Oliva, A. I., Font, D., Sarmentero, M. Á., Álvarez-Bercedo, P., López-Valbuena, J. M., Pericàs, M. A., Enrech, R., Montero, A., Yeste, S., Vidal-Torres, A., Álvarez, I., Pérez, P., Cendán, C. M., Cobos, E. J., Vela, J. M., & Almansa, C

Translational Studies on Anti-Atrial Fibrillatory Action of Oseltamivir by its in vivo and in vitro Electropharmacological Analyses

Author(s): Kambayashi, R., Izumi-Nakaseko, H., Goto, A., Tsurudome, K., Ohshiro, H., Izumi, T., Hagiwara-Nagasawa, M., Chiba, K., Nishiyama, R., Oyama, S., Nunoi, Y., Takei, Y., Matsumoto, A., Sugiyama, A., Zarros, A., Kolb, I., & Heijman, J.

Translational Studies on Anti-Atrial Fibrillatory Action of Oseltamivir by its in vivo and in vitro Electropharmacological Analyses

Author(s): Ryuichi Kambayashi, Hiroko Izumi-Nakaseko, Ai Goto, Kazuya Tsurudome, Hironori Ohshiro, Taku Izumi, Mihoko Hagiwara-Nagasawa, Koki Chiba, Ryota Nishiyama, Satomi Oyama, Yoshio Nunoi, Yoshinori Takei, Akio Matsumoto, Atsushi Sugiyama

Transfection methods for high-throughput cellular assays of voltage-gated calcium and sodium channels involved in pain

Author(s): Md. Mahadhi Hasan, Lotten Ragnarsson, Fernanda C. Cardoso, Richard J. Lewis

Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria

Author(s): Colin K. Skepper, Duncan Armstrong, Carl J. Balibar, Daniel Bauer, Cornelia Bellamacina, Bret M. Benton, Dirksen Bussiere, Gianfranco De Pascale, Javier De VicenteJavier De Vicente, Charles R. Dean, Bhavesh Dhumale, L. Mark Fisher, John Fuller, Mangesh Fulsunder, Lauren M. Holder, Cheng Hu, Bhavin Kantariya, Guillaume Lapointe, Jennifer A. Leeds, Xiaolin Li, Peichao Lu, Anatoli Lvov, Sylvia Ma, Shravanthi Madhavan, Swapnil Malekar, David McKenney, Wosenu Mergo, Louis Metzger, Heinz E. Moser, Daniel Mutnick, Jonas Noeske, Colin Osborne, Ashish Patel, Darshit Patel, Tushar Patel, Krunal Prajapati, Katherine R. Prosen, Folkert Reck, Daryl L. Richie, Alice Rico, Mark R. Sanderson, Shailesh Satasia, William S. Sawyer, Jogitha Selvarajah, Nirav Shah, Kartik Shanghavi, Wei Shu, Katherine V. Thompson, Martin Traebert, Anand Vala, Lakhan Vala, Dennis A. Veselkov, Jason Vo, Michael Wang, Marcella Widya, Sarah L. Williams, Yongjin Xu, Qin Yue, Richard Zang, Bo Zhou, and Alexey Rivkin

TMEM16A Potentiation: A Novel Therapeutic Approach for the Treatment of Cystic Fibrosis

Author(s): Henry L. Danahay, Sarah Lilley, Roy Fox, Holly Charlton, Juan Sabater, Brian Button, Clive McCarthy, Stephen P. Collingwood and Martin Gosling

The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice

Author(s): Nadia Lybøl von Schoubye, Kristen Frederiksen Uffe Kristiansen, Anders Victor Petersend, Nils Ole Dalby, Morten Grunnet, Henrik Sinda Jensen, Thomas Jespersen, Vikaas S. Sohale, Jean-François Perrier

The Snake with the Scorpion’s Sting: Novel Three-Finger Toxin Sodium Channel Activators from the Venom of the Long-Glanded Blue Coral Snake

Author(s): Daryl C. Yang 1,2,†, Jennifer R. Deuis 3,†, Daniel Dashevsky 2,†, James Dobson 2,†, Timothy N. W. Jackson 2, Andreas Brust 3, Bing Xie 4, Ivan Koludarov 2, Jordan Debono 2, Iwan Hendrikx 2, Wayne C. Hodgson 1, Peter Josh 5, Amanda Nouwens 5, Gregory J. Baillie 3, Timothy J. C. Bruxner 3, Paul F. Alewood 3, Kelvin Kok Peng Lim 6, Nathaniel Frank 7, Irina Vetter 3,8,* and Bryan G. Fry 2,*

The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis

Author(s): Vinayak Singh†, Stefano Donini‡, Angela Pacitto§, Claudia SalaΔ, Ruben C. HartkoornΔ, Neeraj DharΔ, Gyorgy Keri⊥, David B. Ascher§, Guillaume Mondésert#, Anthony VocatΔ, Andréanne LupienΔ, Raphael SommerΔ, Hélène Vermet#, Sophie Lagrange#, Joe Buechler⊗, Digby F. Warner†, John D. McKinneyΔ, Janos Pato⊥, Stewart T. ColeΔ, Tom L. Blundell§, Menico Rizzi‡, and Valerie Mizrahi*†

The Glycine Transport Inhibitor Bi 425809 Restores Translatable EEG Deficits in an Acute Mouse Model for Schizophrenia-Related Sensory Processing and Cortical Network Dysfunction

Author(s): Schuelert, N., Dorner-Ciossek, C., & Rosenbrock, H.

The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6

Author(s): Mathilde R. Israel, Panumart Thongyoo, Jennifer R. Deuis, David J. Craik, Irina Vetter, Thomas Durek

The development of automated patch clamp assays for canonical transient receptor potential channels TRPC3, 6, and 7

Author(s): McPate M, Bhalay G, Beckett M, Fairbrother S, Gosling M, Groot-Kormelink PJ, Lane R, Kent T, Van Diepen MT, Tranter P, Verkuyl JM.

Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K+ Channels in Pigs

Journal: Circulation: Arrhythmia and Electrophysiology
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Author(s): Jonas Goldin Diness, Lasse Skibsbye, Rafel Simó-Vicens, Joana Larupa Santos, Pia Lundegaard, Carlotta Citerni, Daniel Rafael Peter Sauter, Sofia Hammami Bomholtz, Jesper Hastrup Svendsen, Søren-Peter Olesen, Ulrik S. Sørensen, Thomas Jespersen, Morten Grunnet, Bo Hjorth Bentzen

Synthetic resin acid derivatives selectively open the hKV7.2/7.3 channel and prevent epileptic seizures

Author(s): Ottosson, N. E., Ejneby, M. S., Wu, X., Estrada-Mondragón, A., Nilsson, M., Karlsson, U., Schupp, M., Rognant, S., Jepps, T. A., Konradsson, P., & Elinder, F.

Synthesis of Pseudellone Analogs and Characterization as Novel T-type Calcium Channel Blockers

Author(s): Dan Wang, Pratik Neupane, Lotten Ragnarsson, Robert J. Capon and Richard J. Lewis

Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139

Author(s): Allen T. Hopper*, Martin Juhl, Jorrit Hornberg, Lassina Badolo, John Paul Kilburn, Annemette Thougaard, Gennady Smagin, Dekun Song, Londye Calice, Veena Menon, Elena Dale, Hong Zhang, Manuel Cajina, Megan E. Nattini, Adarsh Gandhi, Michel Grenon, Ken Jones, Tanzilya Khayrullina, Gamini Chandrasena, Christian Thomsen, Stevin H. Zorn, Robb Brodbeck, Suresh Babu Poda, Roland Staal, and Thomas Möller

Synthesis and Biological Evaluation of Novel Olean-28,13?- lactams as Potential Anti-prostate Cancer Agents

Author(s): Yong Ai†‡, Yang Hu†, Fenghua Kang†‡, Yisheng Lai†‡, Yanju Jia†, Zhangjian Huang*†‡, Sixun Peng†‡, Hui Ji*†, Jide Tian§, and Yihua Zhang*†‡

Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors

Author(s): Daowei Huang, Lei Huang, Qingwei Zhang, Jianqi Li a

Synthesis and Biological Evaluation of Five‐Atom‐Linker‐Based Arylpiperazine Derivatives with an Atypical Antipsychotic Profile

Author(s): Chunhui Wu, Yu Wang, Feipu Yang, Wenqiang Shi, Zhen Wang, Ling He, Yang He, Jingshan Shen

Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect

Author(s): Mingshuo Xu, Yu Wang, Feipu Yang, Chunhui Wu, Zhen Wang, Bin Ye, Xiangrui Jiang, Qingjie Zhao, JianfengLi, Yongjian Liu, Junchi Zhang, Guanghui Tian, Yang He, Jingshan Shen, Hualiang Jiang

Study of TRP Channels by Automated Patch Clamp Systems

Author(s): Morten Sunesen, Rasmus B Jacobsen

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain

Author(s): Steven J. McKerrall, Teresa Nguyen, Kwong Wah Lai, Philippe Bergeron, Lunbin Deng, Antonio Di Pasquale, Jae H. Chang, Jun Chen, Tania Chernov-Rogan, David H. Hackos, Jonathan Maher, Daniel F. Ortwine, Jodie Pang, Jian Payandeh, William R. Proctor, Shannon D. Shields, Jennifer Vogt, Pengfei Ji, Wenfeng Liu, Elisa Ballini, Lilia Schumann, Glauco Tarozzo, Girish Bankar, Sultan Chowdhury, Abid Hasan, J. P. Johnson Jr., Kuldip Khakh, Sophia Lin, Charles J. Cohen, Christoph M. Dehnhardt, Brian S. Safina, Daniel P. Sutherlin

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Author(s): FangZhu, Yuji Wang, Qian Du, Wenxiang Ge, Zhanhui Li, Xu Wang, Chunyan Fu, Lusong Luo, Sheng Tian, Haikuo Ma, Jiyue Zheng, Yi Zhang, Xiaotian Sun, Sudan He, Xiaohu Zhang

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Author(s): Fang Zhu, Yujie Wang, Qian Du, Wenxiang Ge, Zhanhui Li, Xu Wang, Chunyan Fu, Lusong Luo, Sheng Tian, Haikuo Ma, Jiyue Zheng, Yi Zhang, Xiaotian Sun, Sudan He, Xiaohu Zhang

Structural optimization of aminopyrimidine-based CXCR4 antagonists

Author(s): FangZhu, Yujie Wang, Qian Du, Wenxiang Ge, Zhanhui Li, Xu Wang, Chunyan Fu, Lusong Luo, Sheng Tian, Haikuo Ma, JiyueZheng, Yi Zhang, XiaotianSun, Sudan He, Xiaohu Zhang

Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth

Author(s): Peter C. Ray, Margaret Huggett, Penelope A. Turner, Malcolm Taylor, Laura A. T. Cleghorn, Julie Early, Anuradha Kumar, Shilah A. Bonnett, Lindsay Flint, Douglas Joerss, James Johnson, Aaron Korkegian, Steven Mullen, Abraham L. Moure, Susan H. Davis, Dinakaran Murugesan, Michael Mathieson, Nicola Caldwell, Curtis A. Engelhart, Dirk Schnappinger, Ola Epemolu, Fabio Zuccotto, Jennifer Riley, Paul Scullion, Laste Stojanovski, Lisa Massoudi, Gregory T. Robertson, Anne J. Lenaerts, Gail Freiberg, Dale J. Kempf, Thierry Masquelin, Philip A. Hipskind, Joshua Odingo, Kevin D. Read, Simon R. Green, Paul G. Wyatt, and Tanya Parish

Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Donglin Guo & Stephen Jenkinson

Selective Nav1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain

Author(s): Girish Bankar, Samuel J. Goodchild, Sarah Howard, Karen Nelkenbrecher, Matthew Waldbrook, Michelle Dourado, Noah G. Shuart, Sophia Lin, Clint Young, Zhiwei Xie, Kuldip Khakh, Elaine Chang, Luis E. Sojo, Andrea Lindgren, Sultan Chowdhury, Shannon Decker, Michael Grimwood, Jean-Christophe Andrez, Christoph M. Dehnhardt, Jodie Pang, Jae H. Chang, Brian S. Safina, Daniel P. Sutherlin, James P. Johnson, Jr., David H. Hackos, C. Lee Robinette, and Charles J. Cohen

Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators

Author(s): Kenneth Walsh

Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators

Journal: SLAS Discovery: Advancing the Science in Drug Discovery
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Author(s): Kenneth B. Walsh

Screening system for drug-induced arrhythmogenic risk combining a patch clamp and heart simulator

Author(s): Jun-ichi Okada1,2,*, Takashi Yoshinaga3, Junko Kurokawa4, Takumi Washio1,2, Tetsushi Furukawa4, Kohei Sawada3, Seiryo Sugiura1,2 and Toshiaki Hisada1,2

Screening strategies for the discovery of ion channel monoclonal antibodies

Author(s): Caroline S. Colley, Elizabeth England, John E. Linley, Trevor C. I. Wilkinson

Screening assay protocols targeting the Nav1.7 Channel using Qube, a high-throughput automated patch clamp system

Author(s): Binbin Qian, Sung H Park, Weifeng Yu

Screening Assay Protocols Targeting the Nav1.7 Channel Using Qube High‐Throughput Automated Patch‐Clamp System

Author(s): Binbin Qian, Sung Hoon Park and Weifeng Yu

Scaffold Hopping Toward Agomelatine: Novel 3, 4-Dihydroisoquinoline Compounds as Potential Antidepressant Agents

Author(s): Yang Yang, Wei Ang, Haiyue Long, Ying Chang, Zicheng Li, Liangxue Zhou, Tao Yang, Yong Deng & Youfu Luo

Role of High-Throughput Electrophysiology in Drug Discovery

Author(s): Chang Liu, Tianbo Li, and Jun Chen

Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr–/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator

Author(s): Brandon S. Martin 1), Gabriel Martinez-Botella 2), Carlos M. Loya 2), Francesco G. Salituro 2), Albert J. Robichaud 2), Molly M. Huntsman 3), Mike A. Ackley 2), James J. Doherty 2),* and Joshua G. Corbin 1)

Recombinant production, bioconjugation and membrane binding studies of Pn3a, a selective Nav1.7 inhibitor

Author(s): Gagan Sharma, Jennifer R. Deuis, Xinying Jia, Alexander Mueller, Irina Vetter, Mehdi Mobli

Recombinant Production , Bioconjugation and Membrane Binding Studies of Pn3a , a Selective Nav1.7 Inhibitor

Author(s): Gagan Sharma, Jennifer R. Deuis, Xinying Jia, Alexander Mueller, Irina Vetter, Mehdi Mobli

Rational engineering defines a molecular switch that is essential for activity of spider-venom peptides against the analgesics target Nav1.7

Author(s): Julie K Klint, Yanni K. Y. Chin, and Mehdi Mobli

QPatch: the past, present and future of automated patch clamp

Author(s): Chris Mathes

QPatch: the missing link between HTS and ion channel drug discovery.

Journal: Combinatorial Chemistry & High Throughput Screening
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Author(s): Chris Mathes*,1, Søren Friis 2, Michael Finley 3 and Yi Liu 3

Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome

Author(s): Enza Lacivita, Mauro Niso, Madia Letizia Stama, Anna Arzuaga, Concetta Altamura, Lara Costa, Jean-François Desaphy, Michael E. Ragozzino, Lucia Ciranna, Marcello Leopoldo

Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome

Author(s): Enza Lacivita, Mauro Niso, Madia Letizia Stama, Anna Arzuaga, Concetta Altamura, Lara Costad, Jean-François Desaphy, Michael E. Ragozzino, Lucia Ciranna, Marcello Leopoldo

Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs

Author(s): Paula Katavolos, Gary Cain, Cindy Farman, F. Anthony Romero, Steven Magnuson, Justin Q. Ly, Edna F. Choo, Anand Kumar Katakam, Roxanne Andaya, Jonathan Maher

Positive allosteric modulators of α7 nicotinic acetylcholine receptors affect neither the function of other ligand- and voltage-gated ion channels and acetylcholinesterase, nor β-amyloid content

Journal: The International Journal of Biochemistry & Cell Biology
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Author(s): Hugo R. Ariasa, Federica Ravazzinib, Katarzyna M. Targowska-Dudac, Agnieszka A. Kaczord, e, Dominik Feuerbachf, Juan C. Boffig, Piotr Draczkowskid, Dirk Montagh, Brandon M. Browni, Ana Belén Elgoyheng, Krzysztof Jozwiakc, Giulia Puiab

Porphyrin derivatives as potent and selective blockers of neuronal Kv1 channels

Author(s): D. Daly a), A. Al-Sabi b), G. K. Kinsella c), K. Nolan a) and J. O. Dolly b)

Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brainstem neurons

Author(s): Maile Reed Brown 1), Lynda El-Hassar 1), Yalan Zhang 1), Giuseppe Alvaro 2), Charles H Large 2), and Leonard K. Kaczmarek 3)

Pharmacological screening technologies for venom peptide discovery

Author(s): Prashanth JR(1, Hasaballah N(1, Vetter I(2

Pharmacological Inhibition of the Voltage-Gated Sodium Channel NaV1.7 Alleviates Chronic Visceral Pain in a Rodent Model of Irritable Bowel Syndrome

Journal: ACS Pharmacology & Translational Science
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Author(s): Jiang, Y., Castro, J., Blomster, L. V., Agwa, A. J., Maddern, J., Schober, G., Herzig, V., Chow, C. Y., Cardoso, F. C., França, P. D. D. S., Gonzales, J., Schroeder, C. I., Esche, S., Reiner, T., Brierley, S. M., & King, G. F.

Pharmacological characterisation of the highly Nav1.7 selective spider venom peptide Pn3a

Author(s): Jennifer R. Deuis, Zoltan Dekan, Joshua S. Wingerd, Jennifer J. Smith, Nehan R. Munasinghe, Rebecca F. Bhola 2), Wendy L. Imlach, Volker Herzig, David A. Armstrong, K. Johan Rosengren, Frank Bosmans, Stephen G. Waxman, Sulayman D. Dib-Hajj, Pierre Escoubas, Michael S. Minett, Macdonald J. Christie, Glenn F. King, Paul F. Alewood, Richard J. Lewis, John N. Wood & Irina Vetter

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I

Author(s): Kirsten L. McMahon, Bryan Tay, Jennifer R. Deuis, Brian S.Tanaka, Steve Peigneur, Ai-Hua Jin, Jan Tytgat, Stephen G. Waxman, Sulayman D. Dib-Hajj, Irina Vetter, Christina I. Schroeder

Pharmacological activity and NMR solution structure of the leech peptide HSTX-I

Author(s): Kirsten L. McMahon, Bryan Tay, Jennifer R. Deuis, Brian S. Tanaka, Steve Peigneur, Ai-Hua Jin, Jan Tytgat, Stephen G. Waxman, Sulayman D. Dib-Hajj, Irina Vetter, Christina I. Schroeder

pH-dependent inhibition of K2P3.1 prolongs atrial refractoriness in whole hearts

Author(s): Mark A. Skarsfeldt, Thomas A. Jepps, Sofia H. Bomholtz, Lea Abildgaard, Ulrik S. Sørensen, Emilie Gregers, Jesper H. Svendsen

Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation

Author(s): Santoshi Billakota, J. Michael Andresen, Bryant C. Gay, Gregory R. Stewart, Nikolai B. Fedorov, Aaron C. Gerlach, Orrin Devinsky

Perforated Whole-Cell Recordings in Automated Patch Clamp Electrophysiology

Author(s): Rosholm, K. R., Boddum, K., & Lindquist, A

Patch clamping by numbers

Author(s): Claire Wood 1, Gareth J. Waldron* 1, Christine Williams 2, Gareth J. Waldron 2

Patch clamp electrophysiology steps up a gear

Author(s): Derek J. Trezise

Optogenetics and Optical Tools in Automated Patch Clamping

Author(s): Boddum, K., Skafte-Pedersen, P., Rolland, J. F., & Wilson, S

NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions

Author(s): Nausch B, Rode F, Jørgensen S, Nardi A, Korsgaard MP, Hougaard C, Bonev AD, Brown WD, Dyhring T, Strøbæk D, Olesen SP, Christophersen P, Grunnet M, Nelson MT, Rønn LC.

Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity

Author(s): Kazuyuki Kuramoto, Yuki Sawada, Tomohiro Yamada, Takeyuki Nagashima, Kei Ohnuki, Takashi Shin

Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity

Author(s): Kazuyuki Kuramoto, Yuki Sawada, Tomohiro Yamada, Takeyuki Nagashima, Kei Ohnuki, Takashi Shin

Novel Chitohexaose Analog Protects Young and Aged mice from CLP Induced Polymicrobial Sepsis

Author(s): Pragnya Das, Santosh K. Panda, Beamon Agarwal, Sumita Behera, Syed M. Ali, Mark E. Pulse, Joseph S. Solomkin, Steven M. Opal, Vineet Bhandari & Suchismita Acharya

Novel bacterial topoisomerase inhibitors derived from isomannide

Author(s): Antony Okumu, Yanran Lua, Sheri Dellos-Nolan, Jonathan L. Papa, Bryan Koci, Nicholas T. Cockroft, Judith Gallucci, Daniel J.Wozniak, Jack C.Yalowich, Mark J. Mitton-Frya

Novel bacterial topoisomerase inhibitors derived from isomannide

Author(s): Antony Okumu, Yanran Lu, Sheri Dellos-Nolan, Jonathan L. Papa, Bryan Koci, Nicholas T. Cockroft, Judith Gallucci, Daniel J. Wozniak, Jack C. Yalowich, Mark J. Mitton-Fry

New V1a Receptor Antagonist. Part 2. Identification and Optimization of Triazolobenzazepines

Journal: Bioorganic & Medicinal Chemistry Letters
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Author(s): Éva Bozó, Ferenc Baska, Klára Lövei, Gábor Szántó, Katalin Domány-Kovács, Dalma Kurkó, Krisztina Szondiné Kordás, Teodóra Szokoli, Imre Bata

New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1

Author(s): Nichole Coleman, Brandon M. Brown, Aida Oliván-Viguera, Vikrant Singh, Marilyn M. Olmstead, Marta Sofia Valero, Ralf Köhler and Heike Wulff

Multiple sodium channel isoforms mediate the pathological effects of Pacific ciguatoxin-1

Author(s): Marco C. Inserra, Mathilde R. Israel, Ashlee Caldwell, Joel Castro, Jennifer R. Deuis, Andrea M. Harrington, Angelo Keramidas, Sonia Garcia-Caraballo, Jessica Maddern, Andelain Erickson, Luke Grundy, Grigori Y. Rychkov, Katharina Zimmermann, Richard J. Lewis, Stuart M. Brierley & Irina Vetter

Modulation of P2X3 and P2X2/3 Receptors by Monoclonal Antibodies

Author(s): Anatoly Shcherbatko‡12, Davide Foletti‡1, Kris Poulsen‡1, Pavel Strop‡, Guoyun Zhu‡, Adela Hasa-Moreno‡, Jody Melton Witt‡, Carole Loo‡, Stellanie Krimm‡, Ariel Pios‡, Jessica Yu‡, Colleen Brown‡, John K. Lee§, Robert Stroud¶, Arvind Rajpal‡ and David Shelton‡

Modulation of Lymphocyte Potassium Channel KV1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin

Author(s): Seow Theng Ong,* Saumya Bajaj, Mark R. Tanner, Shih Chieh Chang, Bankala Krishnarjuna, Xuan Rui Ng, Rodrigo A. V. Morales, Ming Wei Chen, Dahai Luo, Dharmeshkumar Patel, Sabina Yasmin, Jeremy Jun Heng Ng, Zhong Zhuang, Hai M. Nguyen, Abbas El Sahili, Julien Lescar, Rahul Patil, Susan A. Charman, Edward G. Robins, Julian L. Goggi, Peng Wen Tan, Pragalath Sadasivam, Boominathan Ramasamy, Siddana V. Hartimath, Vikas Dhawan, Janna Bednenko, Paul Colussi, Heike Wulff, Michael W. Pennington, Serdar Kuyucak, Raymond S. Norton, Christine Beeton, and K. George Chandy*

Modulation of Lymphocyte Potassium Channel Kv1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin

Author(s): Seow Theng Ong, Saumya Bajaj, Mark R. Tanner, Shih Chieh Chang, Bankala Krishnarjuna, Xuan Rui Ng, Rodrigo A. V. Morales, Ming Wei Chen, Dahai Luo, Dharmeshkumar Patel, Sabina Yasmin, Jeremy Jun Heng Ng, Zhong Zhuang, Hai M. Nguyen, Abbas El Sahili, Julien Lescar, Rahul Patil, Susan A. Charman, Edward G. Robins, Julian L. Goggi, Peng Wen Tan, Pragalath Sadasivam, Boominathan Ramasamy, Siddana V. Hartimath, Vikas Dhawan, Janna Bednenko, Paul Colussi, Heike Wulff, Michael W. Pennington, Serdar Kuyucak, Raymond S. Norton, Christine Beeton, and K. George Chandy

MICE Models: Superior to the HERG Model in Predicting Torsade de Pointes

Author(s): James Kramer 1*, Carlos A. Obejero-Paz 1*, Glenn Myatt 2, Yuri A. Kuryshev 1, Andrew Bruening-Wright 1, Joseph S. Verducci 3 & Arthur M. Brown 1

Mashiningan improves opioid-induced constipation in rats by activating cystic fibrosis transmembrane conductance regulator chloride channel

Journal: Journal of Pharmacology and Experimental Therapeutics
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Author(s): Yumi Harada, Seiichi Iizuka, Yayoi Saegusa, Sachiko Mogami, Naoki Fujitsuka and Tomohisa Hattori

Mapping the Molecular Surface of the Analgesic Nav1.7-Selective Peptide Pn3a Reveals Residues Essential for Membrane and Channel Interactions

Author(s): Alexander Mueller, Zoltan Dekan, Quentin Kaas, Akello J. Agwa, Hana Starobova, Paul F. Alewood, Christina I. Schroeder, Mehdi Mobli, Jennifer R. Deuis, and Irina Vetter

Manipulation of a spider peptide toxin alters its affinity for lipid bilayers and potency and selectivity for voltage-gated sodium channel subtype

Author(s): Akello J. Agwa, Poanna Tran, Alexander Mueller, Hue N. T. Tran, Jennifer R. Deuis, Mathilde R. Israel, Kirsten L. McMahon, David J. Craik, Irina Vetter and Christina I. Schroeder

Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors

Author(s): Fumihito Ushiyama, Hideaki Amada, Yasuhiro Mihara, Tomoki Takeuchi, Nozomi Tanaka-Yamamoto Masashi Mima, Masafumi Kamitani, Reiko Wada, Yunoshin Tamura, Mayumi Endo, Aiko Masuko, Iichiro Takata, Kosuke Hitaka, Hiroyuki, Sugiyama, Norikazu Ohtake

Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532

Author(s): Fumihito Ushiyama, Hajime Takashima, Yohei Matsuda, Yuya Ogata, Naoki Sasamoto, Risa Kurimoto-Tsuruta, Kaori Ueki, Nozomi Tanaka-Yamamoto, Mayumi Endo, Masashi Mima, Kiyoko Fujita, Iichiro Takata, Satoshi Tsuji, Haruhiro Yamashita Hirotoshi, Okumura Katsumasa, Otake, Hiroyuki Sugiyama

Isoliquiritigenin, an active ingredient of Glycyrrhiza, elicits antinociceptive effects via inhibition of Nav channels

Journal: Naunyn-Schmiedeberg's Archives of Pharmacology
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Author(s): Yuichi Miyamura, Suzuro Hitomi, Yuji Omiya, Izumi Ujihara, Shoichiro Kokabu, Yasuhiro Morimoto & Kentaro Ono

Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach

Journal: Bioorganic & Medicinal Chemistry Letters
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Author(s): Johan Kajanus, Ingemar Jacobson, Annika Åstrand (b., Roine I. Olsson, Ulrik Gran, Annika Björe, Ola Fjellström (a., Öjvind Davidsson, Hans Emtenäs, Anders Dahlén, Boel Löfberg, Zhong-Qing Yuan, Johan Sundell, Johan Cassel, Jonna Gyll, Tommy Iliefski, Ågot Högberg, Emma Lindhardt, Jesper Malmberg

Ion Channels and Relevant Drug Screening Approaches

Author(s): Joseph G. McGivern, Mei Ding

Ion Channels and Relevant Drug Screening Approaches

Journal: SLAS DISCOVERY: Advancing the Science of Drug Discovery
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Author(s): Joseph G. McGivern and Mei Ding

Ion channel screening technologies today

Author(s): Georg C. Terstappen

Intracellular Calcium Mobilization in Response to Ion Channel Regulators via a Calcium-Induced Calcium Release Mechanism

Journal: The Journal of Pharmacology and Experimental Therapeutics
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Author(s): Terry Petrou, Hervør L. Olsen, Christopher Thrasivoulou, John R. Masters, Jonathan F. Ashmore, and Aamir Ahmed

Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor

Author(s): M. Flinspach, Q. Xu, A. D. Piekarz, R. Fellows, R. Hagan, A. Gibbs, Y. Liu, R. A. Neff, J. Freedman, W. A. Eckert, M. Zhou, R. Bonesteel, M. W. Pennington, K. A. Eddinger, T. L. Yaksh, M. Hunter, R. V. Swanson & A. D. Wickenden

Inhibitory effects of cannabidiol on voltage-dependent sodium currents

Author(s): Mohammad-Reza Ghovanloo, Noah Gregory Shuart, Janette Mezeyova, Richard A Dean, Peter C Ruben and Samuel J Goodchild

Inhibitory Effect of Anti-Seizure Medications on Ionotropic Glutamate Receptors: Special Focus on AMPA Receptor Subunits

Author(s): Kazuyuki Fukushima, Ken Hatanaka Koji Sagane, KatsutoshiIdo

Inhibition of the potassium channel KCa3.1 by senicapoc reverses tactile allodynia in rats with peripheral nerve injury

Journal: Volume 795, 15 January 2017, Pages 1–7
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Author(s): Roland G.W. Staala, Tanzilya Khayrullinaa, Hong Zhanga, Scott Davisb, Shaun M. Fallona, Manuel Cajinac, Megan E. Nattinic, Andrew Hub, Hua Zhouc, Suresh Babu Podac, Stevin Zorna, Gamini Chandrasenac, Elena Dalea, Brian Campbella, Lars Christian Biilmann Rønnd, Gordon Munrod, Thomas Mӧllera

Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia

Journal: Pharmacology of Ion Channels and Channelopathies
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Author(s): Jonas Goldin Diness, Lea Abildgaard, Sofia Hammami Bomholtz, Mark Alexander Skarsfeldt, Nils Edvardsson, Ulrik S. Sørensen, Morten Grunnet and Bo Hjorth Bentzen

Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia

Author(s): Jonas Goldin Diness, Lea Abildgaard, Sofia Hammami Bomholtz, Mark Alexander Skarsfeldt, Nils Edvardsson, Ulrik S. Sørensen, Morten Grunnet and Bo Hjorth Bentzen

In Vitro and in Vivo Characterization of Lu AA41178: A Novel, Brain Penetrant, Pan-Selective Kv7 Potassium Channel Opener with Efficacy in Preclinical Models of Epileptic Seizures and Psychiatric Disorders

Author(s): MortenGrupe, Bo Hjorth Bentzen, Tau Benned-Jensen, Vibeke Nielsen, Kristen Frederiksen, Henrik Sindal Jensen, Anne-Marie Jacobsen, Lasse Skibsbye, Anette Graven Sams, Morten Grunnet, Mario Rottländer, Jesper Frank Bastlund

Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp

Author(s): Sören J. Wacker, Dr. Wiktor Jurkowski, Dr. Katie J. Simmons, Prof. Dr. Colin W. G. Fishwick, Prof. Dr. A. Peter Johnson, Dr. David Madge, Prof. Dr. Erik Lindahl, Dr. Jean‐Francois Rolland, Prof. Dr. Bert L. de Groot

Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel

Author(s): Pamela A. Haile, Linda N. Casillas, Michael J. Bury, John F. Mehlmann, Robert Singhaus, Jr., Adam K. Charnley, Terry V. Hughes, Michael P. DeMartino, Gren Z. Wang, Joseph J. Romano, Xiaoyang Dong, Nikolay V. Plotnikov, Ami S. Lakdawala, Maire A. Convery, Bartholomew J. Votta, David B. Lipshutz, Biva M. Desai, Barbara Swift, Carol A. Capriotti, Scott B. Berger, Mukesh K. Mahajan, Michael A. Reilly, Elizabeth J. Rivera, Helen H. Sun, Rakesh Nagilla, Carol LePage, Michael T. Ouellette, Rachel D. Totoritis, Brian T. Donovan, Barry S. Brown†, Khuram W. Chaudhary†, Peter J. Gough, John Bertin, and Robert W. Marquis

Identification of poly(ADP-ribose)polymerase 1 and 2 (PARP1/2) as targets of andrographolide using an integrated chemical biology approach

Author(s): Li, W., Pan, B., Shi, Y., Wang, M., Han, T., Wang, Q., Duan, G., & Fu, H.

Identification and Electrophysiological Evaluation of 2-Methylbenzamide Derivatives as Nav1.1 Modulators

Author(s): François Crestey§, Kristen Frederiksen§, Henrik S. Jensen§, Kim Dekermendjian§, Peter H. Larsen§, Jesper F. Bastlund§, Dunguo Lu†, Henry Liu†, Charles R. Yang†, Morten Grunnet*§, and Niels Svenstrup*§

Identification and Characterization of ProTx-III [μ-TRTX-Tp1a], a New Voltage-Gated Sodium Channel Inhibitor from Venom of the Tarantula Thrixopelma pruriens

Author(s): Fernanda C. Cardoso, Zoltan Dekan, K. Johan Rosengren, Andelain Erickson, Irina Vetter, Jennifer R. Deuis, Volker Herzig, Paul F. Alewood, Glenn F. King, and Richard J. Lewis

HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor

Author(s): Ledneczki, I., Horváth, A., Tapolcsányi, P., Éles, J., Molnár, K. D., Vágó, I., Visegrády, A., Kiss, L., Szigetvári, Á., Kóti, J., Krámos, B., Mahó, S., Holm, P., Kolok, S., Fodor, L., Thán, M., Kostyalik, D., Balázs, O., Vastag, M., … Némethy, Z.

High-Throughput Screening of Nav1.7 Modulators Using a Giga-Seal Automated Patch Clamp Instrument

Author(s): Chris Chambers, Ian Witton, Cathryn Adams, Luke Marrington and Juha Kammonen

High-Throughput Screen of GluK1 Receptor Identifies Selective Inhibitors with a Variety of Kinetic Profiles Using Fluorescence and Electrophysiology Assays

Author(s): Kelli Solly 1), Rebecca Klein 2), Michael Rudd 3), M. Katharine Holloway 4), Eric N. Johnson 1),*, Darrell Henze 2), Michael F. A. Finley 1)

High-throughput electrophysiology: An emerging paradigm for ion-channel screening and physiology

Author(s): John Dunlop, Mark Bowlby, Ravikumar Peri, Dmytro Vasilyev & Robert Arias

High throughput physiological screening of iPSC-derived cardiomyocytes for drug development

Journal: Biochimica et Biophysica Acta (BBA) - Molecular Cell Research
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Author(s): Juan C. del Álamo a), Derek Lemonsb, c), Ricardo Serrano a), Alex Savchenkob, c, e), Fabio Cerignoli d), Rolf Bodmer c), Mark Mercolab, c, e)

Functional Studies of Sodium Channels: From Target to Compound Identification

Journal: Wiley Online Library DOI: 10.1002/cpph.14
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Author(s): Daniel Bertrand 1), Bruno Biton 2), Thomas Licher 3), Jean-Marie Chambard 2), Christophe Lanneau 2), Michel Partiseti 2), Isabel A. Lefevre 2)

From identification to functional characterization of cyriotoxin-1a, an antinociceptive toxin from the spider Cyriopagopus schioedtei.

Author(s): Gonçalves TC, Benoit E, Kurz M, Lucarain L, Fouconnier S, Combemale S, Jaquillard L, Schombert B, Chambard JM, Boukaiba R, Hessler G, Bohme A, Bialy L, Hourcade S, Béroud R, De Waard M, Servent D, Partiseti M

From High-Throughput Screening to Target Validation: Benzo[d]isothiazoles as Potent and Selective Agonists of Human Transient Receptor Potential Cation Channel Subfamily M Member 5 Possessing In Vivo Gastrointestinal Prokinetic Activity in Rodents

Author(s): Barilli, A., Aldegheri, L., Bianchi, F., Brault, L., Brodbeck, D., Castelletti, L., Feriani, A., Lingard, I., Myers, R., Nola, S., Piccoli, L., Pompilio, D., Raveglia, L. F., Salvagno, C., Tassini, S., Virginio, C., & Sabat, M.

Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization

Author(s): Junior Gonzales, Giacomo Pirovano, Chun Yuen Chow, Paula Demetrio de Souza Franca, Lukas M. Carter, Julie K. Klint, Navjot Guru, Jason S. Lewis, Glenn F. King and Thomas Reiner

Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization

Author(s): Junior Gonzales, Giacomo Pirovano, Chun Yuen Chow, Paula Demetrio de Souza Franca, Lukas M. Carter, Julie K. Klint, Navjot Guru, Jason S. Lewis, Glenn F. King & Thomas Reiner

Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment

Author(s): Seow Theng Ong, Aik Seng Ng, Xuan Rui Ng, Zhong Zhuang, Brandon Han Siang Wong, Praseetha Prasannan, Yee Jiun Kok, Xuezhi Bi, Heesung Shim, Heike Wulff, Kanianthara George Chandy, and Navin Kumar Verma

EST64454: a Highly Soluble σ 1 Receptor Antagonist Clinical Candidate for Pain Management

Author(s): José Luis Díaz, Mónica García, Mónica García, Antoni Torrens, Ana María Caamaño, Juan Enjo, Cristina Sicre, Adriana Lorente, Adriana Port, Ana Montero, Sandra Yeste, Inés Álvarez, Miquel Martín, Rafael Maldonado, Beatriz de laPuente, Alba Vidal-Torres, Cruz Miguel Cendán, José Miguel Vela, and Carmen Almansa

Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition

Author(s): Hue N. T. Tran, Hue N. T. Tran, Poanna Tran, Jennifer R. Deuis, Akello J. Agwa, Alan H. Zhang, Irina Vetter, and Christina I. Schroeder

Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition

Author(s): Hue N. T. Tran, Poanna Tran, Jennifer R. Deuis, Akello J. Agwa, Alan H. Zhang, Irina Vetter and Christina I. Schroeder

Engineering Highly Potent and Selective Microproteins Against Nav1.7 Sodium Channel for Treatment of Pain

Author(s): Anatoly Shcherbatko1, Andrea Rossi1, Davide Foletti2, Guoyun Zhu1, Oren Bogin3, Meritxell Galindo-Casas1, Mathias Rickert4, Adela Hasa-Moreno1, Victor Bartevitch5, Andreas Crameri6, Alexander R. Steiner7, Robert Henningsen7, Avinash Gill8, Jaume Pons1, David L. Shelton1, Arvind Rajpal9 and Pavel Strop1*

Electrophysiological Studies of GABA-A Receptors Using QPatch II, the Next Generation of Automated Patch‐Clamp Instruments

Author(s): Melanie Schupp Sung Hoon Park Binbin Qian Weifeng Yu

Electrophysiological and Pharmacological Characterization of Human Inwardly Rectifying Kir2.1 Channels on an Automated Patch-Clamp Platform

Author(s): Camille Sanson, Brigitte Schombert, Bruno Filoche-Romme, Michel Partiseti and G. Andrees Bohme

Eleclazine exhibits enhanced selectivity for long QT syndrome type 3–associated late Na+ current

Author(s): Nesrine El-Bizri, Cheng Xie, Lynda Liu, James Limberis, Michael Krause, Ryoko Hirakawa, Steven Nguyen, Dennis R. Tabuena, Luiz Belardinelli, Kristopher M.Kahlig

Efficient Enzymatic Ligation of Inhibitor Cystine Knot Spider Venom Peptides: Using Sortase A To Form Double-Knottins That Probe Voltage-Gated Sodium Channel NaV1.7

Author(s): Agwa AJ, Blomster LV, Craik DJ, King GF, Schroeder CI.

Effect of antiarrhythmic drugs on small conductance calcium – activated potassium channels

Author(s): Rafel Simó-Vicensa, Daniel R.P. Sauter, Morten Grunnet, Jonas G. Diness, Bo H. Bentzen

Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis

Author(s): Ana Guardia, Jessica Baiget, Mónica Cacho, Arancha Pérez, Montserrat Ortega-Guerra, Winston Nxumalo, Setshaba D. Khanye, Joaquín Rullas, Fátima Ortega, Elena Jiménez, Esther Pérez-Herrán, María Teresa Fraile-Gabaldón, Jorge Esquivias, Raquel Fernández, Esther Porras-De Francisco, Lourdes Encinas, Marta Alonso, Ilaria Giordano, Cristina Rivero, Juan Miguel-Siles, Javier G. Osende, Katrina A. Badiola, Peter J. Rutledge , Matthew H. Todd, Modesto Remuiñán, and Carlos Alemparte

Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Yevgeniya E. Koshman, Amanda S.Wilsey Brandan M.Bird Aimee L. Endemann Sabine Sadilek, Jessica Treadway, Ruth L. Martin, James S. Polakowski, Gary A.Gintant, Scott W.Mittelstadt

Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Yevgeniya E. Koshman, Amanda S. Wilsey, Brandan M. Bird, Aimee L. Endemann, Sabine Sadilek, Jessica Treadway, Ruth L. Martin, James S. Polakowski, Gary A. Gintant, Scott W. Mittelstadt

Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide are Potent TMEM16A Antagonists that Fully Bronchodilate Airway

Author(s): Kent Miner, Katja Labitzke, Benxian Liu, Paul Wang, Kathryn Henckels, Kevin Gaida, Robin Elliott, Jian Jeffrey Chen, Longbin Liu, Anh Leith, Esther Trueblood, Kelly Hensley, Xing-Zhong Xia, Oliver Homann, Brian Bennett, Mike Fiorino, John Whoriskey, Gang Yu, Sabine Escobar, Min Wong, Teresa L. Born, Alison Budelsky, Mike Comeau, Dirk Smith, Jonathan Phillips, James A. Johnston, Joe McGivern, Kerstin Weikl, David Powers, Karl Kunzelmann, Deanna Mohn, Andreas Hochheimer, John K. Sullivan

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Author(s): Bandita Bagchi, Ahmed Al-Sabi, Seshu Kaza, Dimitri Scholz, Valerie B. O’Leary, J. Oliver Dolly, Saak V. Ovsepian

Disruption of Myelin Leads to Ectopic Expression of KV1.1 Channels with Abnormal Conductivity of Optic Nerve Axons in a Cuprizone-Induced Model of Demyelination

Author(s): Bandita Bagchi, Ahmed Al-Sabi, Seshu Kaza, Dimitri Scholz, Valerie B. O'Leary, J. Oliver Dolly , Saak V. Ovsepian

Discovery, Pharmacological Characterisation and NMR Structure of the Novel µ-Conotoxin SxIIIC, a Potent and Irreversible NaV Channel Inhibitor

Author(s): Kirsten L. McMahon, Hue N.T. Tran, Richard J. Lewis, Irina Vetter and Christina I. Schroeder

Discovery of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor: Scaffold hopping approach

Author(s): István Ledneczki, Pál Tapolcsányi, Eszter Gábor, András Visegrády, Márton Vass, János Éles, Patrik Holm, Anita Horváth, Anikó Pocsai, Sándor Mahó, István Greiner, Balázs Krámos, Zoltán Béni, János Kóti, Anna E. Káncz, Márta Thán, Sándor Kolok, Judit Laszy, Ottilia Balázs, Gyula Bugovits, József Nagy, Mónika Vastag, Ágota Szájli, Éva Bozó, György Lévay, Balázs Lendvai, Zsolt Némethy

Discovery of Methylene Thioacetal-Incorporated α-RgIA Analogues as Potent and Stable Antagonists of the Human α9α10 Nicotinic Acetylcholine Receptor for the Treatment of Neuropathic Pain

Author(s): Zheng, N., Christensen, S. B., Dowell, C., Purushottam, L., Skalicky, J. J., McIntosh, J. M., & Chou, D. H.-C.

Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A4 Hydrolase

Author(s): Christian Markert, Gebhard Thoma, Honnappa Srinivas, Birgit Bollbuck, Rainer M. Lüönd, Wolfgang Miltz, Rudolf Wälchli, Romain Wolf, Jürgen Hinrichs, Christian Bergsdorf, Kamal Azzaoui,b Carlos A. Penno, Kai Klein, Nathalie Wack, Petra Jäger, Franziska Hasler, Christian Beerli, Pius Loetscher, Janet Dawson, Grazyna Wieczorek, Shin Numao, Amanda Littlewood-Evans, and Till A. Röhn

Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties

Author(s): Michael J. Soth, Kang Le, Maria Emilia Di Francesco, Matthew M. Hamilton, Gang Liu, Jason P. Burke, Chris L. Carroll, Jeffrey J. Kovacs, Jennifer P. Bardenhagen, Christopher A. BristowChristopher A. Bristow, Mario Cardozo, Barbara Czako, Elisa de Stanchina, Ningping Feng, Jill R. Garvey, Jason P. Gay, Mary K. Geck Do, Jennifer Greer, Michelle Han, Angela Harris, Zachary Herrera, Sha Huang, Virginia Giuliani, Yongying Jiang, Sarah B. Johnson, Troy A. Johnson, Zhijun Kang, Paul G. Leonard, Zhen Liu, Timothy McAfoos, Meredith Miller, Pietro Morlacchi, Robert A. Mullinax, Wylie S. Palmer, Jihai Pang, Norma Rogers, Charles M. Rudin, Hannah E. Shepard, Nakia D. Spencer, Jay Theroff, Qi Wu, Alan Xu, Ju Anne Yau, Giulio Draetta, Carlo Toniatti, Timothy P. Heffernan, and Philip Jones

Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain

Author(s): Mónica García, Marina Virgili, Mònica Alonso, Carles Alegret, Joan Farran, Begoña Fernández, Magda Bordas, Rosalia Pascual, Javier Burgueño, Alba Vidal-Torres, Antonio R. Fernández de HenestrosaAntonio R. Fernández de Henestrosa, Eva Ayet, Manuel Merlos, Jose Miguel Vela, Carlos R. Plata-Salamán, and Carmen Almansa

Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain

Author(s): Mónica García, Marina Virgili, Mònica Alonso, Carles Alegret, Joan Farran, Begoña Fernández, Magda Bordas, Rosalia Pascual, Javier Burgueño, Alba Vidal-Torres, Antonio R. Fernández de Henestrosa, Eva Ayet, Manuel Merlos, Jose Miguel Vela, Carlos R. Plata-Salamán, and Carmen Almansa

Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Author(s): Jeff A. Zablocki*†, Elfatih Elzein†, Xiaofen Li†, Dmitry O. Koltun†, Eric Q. Parkhill†, Tetsuya Kobayashi†, Ruben Martinez†, Britton Corkey†, Haibo Jiang†, Thao Perry†, Rao Kalla†, Gregory T. Notte†, Oliver Saunders†, Michael Graupe†, Yafan Lu†, Chandru Venkataramani†, Juan Guerrero†, Jason Perry⊥, Mark Osier§, Robert Strickley∥,Gongxin Liu#, Wei-Qun Wang#, Lufei Hu#, Xiao-Jun Li#, Nesrine El-Bizri#, Ryoko Hirakawa#, Kris Kahlig#, Cheng Xie#, Cindy Hong Li#, Arvinder K. Dhalla#, Sridharan Rajamani#, Nevena Mollova‡, Daniel Soohoo‡, Eve-Irene Lepist‡, Bernard Murray‡, Gerry Rhodes‡, Luiz Belardinelli#, and Manoj C. Desai†

Discovery of (S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.

Author(s): Panayiotis A. Procopiou , Niall A. Anderson, John Barrett, Tim N. Barrett, Matthew H. J. Crawford, Brendan J. Fallon, Ashley P. Hancock, Joelle Le, Seble Lemma, Richard P. Marshall, Josie Morrell, John M. Pritchard, James E. Rowedder, Paula Saklatvala, Robert J. Slack, Steven L. Sollis, Colin J. Suckling, Lee R. Thorp, Giovanni Vitulli, and Simon J. F. Macdonald

Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria

Author(s): Lapointe, G., Skepper, C. K., Holder, L. M., Armstrong, D., Bellamacina, C., Blais, J., Bussiere, D., Bian, J., Cepura, C., Chan, H., Dean, C. R., Pascale, G. De, Dhumale, B., Fisher, L. M., Fulsunder, M., Kantariya, B., Kim, J., King, S., Kossy, L., … Rivkin, A.

Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain

Journal: Bioorganic & Medicinal Chemistry Letters
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Author(s): Mark J.Wall, Nalin L.Subasinghe, Michael P.Winters. Mary Lou Lubin, Michael F.A. Finley, Ning Qin Michael, R. Brandt, Michael P.Neeper, Craig R. Schneider, Raymond W.Colburn, Christopher M. Flores, Zhihua Sui

Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi

Author(s): Silmara R. Sousa, Joshua S. Wingerd, Andreas Brust, Christopher Bladen, Lotten Ragnarsson, Volker Herzig, Jennifer R. Deuis, Sebastien Dutertre, Irina Vetter, Gerald W. Zamponi, Glenn F. King, Paul F. Alewood, Richard J. Lewis

Discovery and electrophysiological characterization of SKF-32802; a novel hERG agonist found through a large-scale structural similarity search

Author(s): Brian T. Donovan, Deepak Bandyopadhyay,, Chaya Duraiswami, Christopher J. Nixon, Claire Y. Townsend, Stan F. Martens

Discovery and Characterization of the Potent and Selective P2X4 Inhibitor N-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile

Author(s): Stefan Werner, Stefanie Mesch, Roman C. Hillig , Antonius ter Laak, Julie Klint, Ioana Neagoe, Alexis Laux-Biehlmann, Henrik Dahllöf, Nico Bräuer, Vera Puetter, Reinhard Nubbemeyer, Simone Schulz, Michaela Bairlein, Thomas M. Zollner, Andreas Steinmeyer

Discovery and characterization of ORM‐11372, a novel inhibitor of the sodium‐calcium exchanger with positive inotropic activity

Author(s): Leena Otsomaa, Jouko Levijoki, Gerd Wohlfahrt, Hugh Chapman, Ari-Pekka Koivisto, Kaisa Syrjänen, Tuula Koskelainen, Saara-Elisa Peltokorpi, Piet Finckenberg, Aira Heikkilä, Najah Abi-Gerges, Andre Ghetti, Paul E. Miller, Guy Page, Eero Mervaala, Norbert Nagy, Zsófia Kohajda, Norbert Jost, László Virág, András Varró, Julius Gy. Papp

Direct evidence for high affinity blockade of NaV1.6 channel subtype by huwentoxin-IV spider peptide, using multiscale functional approaches

Author(s): Tânia C. Gonçalves, Rachid Boukaiba, Jordi Molgób, Muriel Amar, Michel Partiseti, Denis Servent, Evelyne Benoit

Differential Free Intracellular Calcium Release by Class II Antiarrhythmics in Cancer Cell Lines

Journal: The Journal of Pharmacology and Experimental Therapeutics
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Author(s): Reyes-Corral M, Sørensen NM, Thrasivoulou C, Dasgupta P, Ashmore JF 1, Ahmed A

Development of the 1,2,4-triazole-based anticonvulsant drug candidates acting on the voltage-gated sodium channels. Insights from in-vivo, in-vitro, and in-silico studies

Author(s): Barbara Kaproń, Jarogniew J. Łuszczki, Anita Płazińska, Agata Siwek, Tadeusz Karcz, Anna Gryboś, Gabriel Nowak, Anna Makuch-Kocka, Katarzyna Walczak, Ewa Langner, Karolina Szalast, Sebastian Marciniak, Magdalena Paczkowska, Judyta Cielecka-Piontek, Lukasz M.Ciesla, Tomasz Plech

Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems

Author(s): Alessandro Grillo, Giulia Chemia Simone Brogi, Margherita Brindisi, Nicola Relitti, Filomena Fezza, Domenico Fazioe, Laura Castelletti, Elisabetta Perdona, Andrea Wong, Stefania Lamponi, Alessandra Pecorelli, Mascia Benedusi, Manuela Fantacci, Massimo Valoti, Giuseppe Valacchihi, Fabrizio Micheli, Ettore Novellino, Giuseppe Campiani Stefania Butini, Mauro Maccarrone, Sandra Gemma

Development of Automated Patch Clamp Technique to Investigate CFTR Chloride Channel Function

Author(s): Arnaud Billet, Lionel Froux, John W. Hanrahan and Frederic Becq

Development of Automated Patch Clamp Assay for Evaluation of α7 Nicotinic Acetylcholine Receptor Agonists in Automated QPatch 16

Author(s): Hao Yuchen 1), Tang Jingshu 2), and Wang KeWei 3)

Development of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves

Author(s): Ahmed Al-Sabi, Declan Daly, Myles Rooney, Cian Hughes, Gemma K. Kinsella, Seshu K.Kaza, Kieran Nolan, J.Oliver Dolly

Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves

Author(s): Ahmed Al-Sabi, Declan Daly, Myles Rooney, Cian Hughes, Gemma K. Kinsella, Seshu K. Kaza, Kieran Nolan, J. Oliver Dolly

Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors

Author(s): Kathryn A. Henckels, David Fong, and Jonathan E. Phillips

Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors

Author(s): Kathryn A. Henckels, David Fong and Jonathan E. Phillips

Development of a QPatch Automated Electrophysiology Assay for Identifying KCa3.1 Inhibitors and Activators

Author(s): David Paul Jenkins 1), Weifeng Yu 2), Brandon M. Brown 1), Lars Damgaard Løjkner 2) and Heike Wulff 1)

Development of a high-throughput fluorescent no-wash sodium influx assay

Author(s): Bryan Tay, Teneale A. Stewart, Felicity M. Davis, Jennifer R. Deuis, Irina Vetter

Developing Molecular Pharmacology of BK Channels for Therapeutic Benefit

Author(s): G.J. Kaczorowski, M.L. Garcia

Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens

Author(s): Kong, Q., Pan, W., Xu, H., Xue, Y., Guo, B., Meng, X., Luo, C., Wang, T., Zhang, S., & Yang, Y.

Design, synthesis, and biological evaluation of fluorinated imidazo[1,2-a]pyridine derivatives with potential antipsychotic activity

Author(s): Monika Marcinkowska, Marcin Kołaczkowskia, Krzysztof Kamińskia, Adam Buckia, Maciej Pawłowskia, Agata Siweka, Tadeusz Karcza, Barbara Mordyla, Gabriela Starowicza, Paulina Kubowicza, Elżbieta Pękalaa, Anna Wesołowskaa, Jerzy Samochowiecb, Paweł Mierzejewskic, Przemyslaw Bienkowskic

Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy

Author(s): Chuantao Zha, Wenjia Deng, Yan Fu, Shuai Tang, Xiaojing Lan, Yan Yea, Yi Su, Lei Jiang, Yi Chen, Ying Huang, Jian Ding, Meiyu Geng, Min Huang, Huixin Wan

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis

Author(s): Linhong Hea, Heying Peia, Chufeng Zhanga, Mingfeng Shao, Dan Li, Mingli Tang, Taijing Wang, Xiaoxin Chen, Mingli Xiang, Lijuan Chen

Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5H-thieno[3′,2’:3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5′-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes

Author(s): Shengbin Zhou(ab1, Yanan Duan(c1, Jiang Wang(ab1, Jin Zhang(c Haifeng Sun(a,b Haowen Jiang(c, Zhanni Gu(ab, Junhua Tong(ab, Jingya Li(a, Jia Li(a, Hong Liu(ab

Design, Synthesis and Biological Activity of Novel 2,3,4,5-Tetra-Substituted Thiophene Derivatives as PI3Kα Inhibitors with Potent Antitumor Activity

Author(s): WeikeLiao, Zhongyuan Wang, Yufei Han, Yinliang Qi, Jiaan Liu, Juan Xie, Ye Tian, Qiancheng Leia, Rui Chen, Ming Sun, Lei Tang, Guowei Gong, Yanfang Zhao

Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity

Author(s): Weike Liao, Zhongyuan Wang, Yufei Han, Yinliang Qi, Jiaan Liu, Juan Xie, Ye Tian, Qiancheng Lei, Rui Chen, Ming Sun, Lei Tang, Guowei Gong, Yanfang Zhao,

Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells

Author(s): James Kramer, Herbert M. Himmel, Anders Lindqvist, Sonja Stoelzle-Feix, Khuram W. Chaudhary, Dingzhou Li, Georg Andrees Bohme, Matthew Bridgland-Taylor, Simon Hebeisen, Jingsong Fan, Muthukrishnan Renganathan, John Imredy, Edward S. A. Humphries, Nina Brinkwirth, Tim Strassmaier, Atsushi Ohtsuki, Timm Danker, Carlos Vanoye, Liudmila Polonchuk, Bernard Fermini, Jennifer Beck Pierson & Gary Gintant

Creation of a new class of radiosensitizers for glioblastoma based on the mibefradil pharmacophore

Author(s): Paradkar, S., Herrington, J., Hendricson, A., Hewawasam, P., Plummer, M., Hoyer, D., Sundaram, R. K., Surovtseva, Y. V., & Bindra, R. S.

Comprehensive in vitro cardiac safety assessment using human stem cell technology: Overview of CSAHi HEART initiative

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Takasuna K1, Asakura K2, Araki S3, Ando H4, Kazusa K5, Kitaguchi T6, Kunimatsu T7, Suzuki S8, Miyamoto N9.

Co-expression of β Subunits with the Voltage-Gated Sodium Channel NaV1.7: the Importance of Subunit Association and Phosphorylation and Their Effects on Channel Pharmacology and Biophysics

Author(s): Sokolov MV, Henrich-Noack P, Raynoschek C, Franzén B, Larsson O, Main M, Dabrowski M

Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels

Author(s): Zidar N1, Žula A1, Tomašič T1, Rogers M2, Kirby RW2, Tytgat J3, Peigneur S3, Kikelj D1, Ilaš J4, Mašič LP5

Chloroquine and hydroxychloroquine provoke arrhythmias at concentrations higher than those clinically used to treat COVID‐19: A simulation study

Author(s): Jun‐ichi Okada, Takashi Yoshinaga, Takumi Washio, Kohei Sawada, Seiryo Sugiura, Toshiaki Hisada

Chemical modulation of Kv7 potassium channels

Author(s): Matteo Borgini, Pravat Mondal, Ruiting Liu and Peter Wipf

Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe

Author(s): Mathilde R. Israel, Thomas S. Dash, Stefanie N. Bothe, Samuel D. Robinson, Jennifer R. Deuis, David J. Craik, Angelika Lampert, Irina Vetter and Thomas Durek

Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe

Author(s): Mathilde R. Israel, Thomas S. Dash, Stefanie N. Bothe, Samuel D. Robinson, Jennifer R. Deuis, David J. Craik, Angelika Lampert, Irina Vetter and Thomas Durek

Characterization of Potassium Channel Modulators with QPatch™ Automated Patch-Clamp Technology: System Characteristics and Performance To cite this article:

Author(s): Jonatan Kutchinsky, Søren Friis, Margit Asmild, Rafael Taboryski, Simon Pedersen, Ras K. Vestergaard, Rasmus B. Jacobsen, Karen Krzywkowski, Rikke L. Schrøder, Trine Ljungstrøm, Nathalie Hélix, Claus B. Sørensen, Morten Bech, and Niels J. Willumsen

Characterization of Endogenous Sodium Channels in the ND7-23 Neuroblastoma Cell Line: Implications for Use as a Heterologous Ion Channel Expression System Suitable for Automated Patch Clamp Screening

Author(s): Marc Rogers 1, Nace Zidar 2 Danijel Kikelj 2 and Robert W. Kirby 1

Characterization of compounds on nicotinic acetylcholine receptor alpha7 channels using higher throughput electrophysiology

Author(s): S. Friis a), C. Mathes a,∗), M. Sunesen a), M.R. Bowlby b), J. Dunlop a)

Characterisation of δ-Conotoxin TxVIA as a Mammalian T-Type Calcium Channel Modulator

Author(s): Dan Wang, S.W.A. Himaya, Jean Giacomotto, Md. Mahadhi Hasan, Fernanda C. Cardoso, Lotten Ragnarsson and Richard J. Lewis

Cell volume and membrane stretch independently control K+ channel activity

Author(s): Sofia Hammami 1,2), Niels J. Willumsen 1), Hervør L. Olsen 3), Francisco J. Morera 4), Ram´on Latorre 4) and Dan A. Klaerke 2)

Cardiotoxic Potential of Hydroxychloroquine, Chloroquine and Azithromycin in Adult Human Primary Cardiomyocytes

Author(s): Pierre Jordaan, Bérengère Dumotier, Martin Traebert, Paul E Miller, Andre Ghetti, Laszlo Urban, Najah Abi-Gerges

Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells: An In-Vitro Model to Predict Cardiac Effects of Drugs

Journal: Journal of Biomedical Science and Engineering
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Author(s): Romain Sube, Eric A. Ertel

Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation

Journal: Journal of Pharmacological and Toxicological Methods
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Author(s): Stephen Jenkinson, Asser Bassyouni, Jason Cordes, Bernard Fermini, Donglin Guo, David M.Potter, David S.Ramirez, Jill Steidl-Nichols, Sunny Sun, ToddWisialowski

Cardiac safety assessment with motion field imaging analysis of human iPS cell-derived cardiomyocytes is improved by an integrated evaluation with cardiac ion channel profiling

Author(s): Isobe T, Honda M, Komatsu R, Tabo M

Cannabidiol Inhibits Multiple Cardiac Ion Channels and Shortens Ventricular Action Potential Duration in Vitro

Author(s): Marguerite Le Marois, Véronique Ballet, Camille Sanson, Magali-Anne Maizières, Thierry Carriot, Céline Chantoiseau, Michel Partiseti, Georg Andrees Bohme

Cancer as a channelopathy: ion channels and pumps in tumor development and progression

Author(s): Alisa Litan and Sigrid A. Langhans

Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling

Author(s): Adrian Britschgia, Anke Billb, Heike Brinkhausa, Christopher Rothwell, Ieuan Clay, Stephan Duss, Michael Rebhan, Pichai Raman, Chantale T. Guy, Kristie Wetzel, Elizabeth George, M. Oana Popa, Sarah Lilley, Hedaythul Choudhury, Martin Gosling, Louis Wang, Stephanie Fitzgerald, Jason Borawski, Jonathan Baffoe, Mark Labow, L. Alex Gaither, and Mohamed Bentires-Al

Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned

Author(s): Ryan Choi, Matthew A. Hulverson, Wenlin Huang, Rama S.R. Vidadala, Grant R.Whitman, Lynn K.Barrett, Deborah A. Schaefer, Dana P.Betzer, Michael W. Riggs, J. Stone Doggett, Andrew Hemphill, Luis Miguel Ortega-Morag Molly C. McCloskey, Samuel L.M. Arnold, Robert C.Hackmanhi, Kennan C.Marsh, James J. Lynch, Gail M. Freiberg, Bruce E. Leroy, Dale J.Kempf, Robert K.M.Choy, Eugenio L .de Hostos, Dustin J.Maly, Erkang Fan, Kayode K. Ojo, Wesley C. Van Voorhis

Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands

Author(s): Dorota Lazewska (a, Maria Kaleta(a, J. Stephan Schwed(b, Tadeusz Karcz(a, Szczepan Mogilski(c, Gniewomir Latacz(a, Agnieszka Olejarz(a, AgataSiwek(d, Monika Kubacka(c, Annamaria Lubelska(a, Ewelina Honkisz(a, Jadwiga Handzlik(a, Barbara Filipek(c, HolgerStark(b, Katarzyna Kieć-Kononowicz(a

Biological Profiling of Coleoptericins and Coleoptericin-Like Antimicrobial Peptides from the Invasive Harlequin Ladybird Harmonia axyridis

Journal: Advances in Experimental Medicine and Biology
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Author(s): Rolf Hirsch, Jochen Wiesner, Alexander Marker, Armin Bauer, Peter E. Hammann, Andreas Vilcinskas

Benzothiophenes as Potent Analgesics Against Neuropathic Pain

Author(s): Saurabh Yadav, Vishnu Kumar Dwivedi, Sarika Gupta, Avadhesha Surolia

Automated Planar Electrode Electrophysiology in Drug Discovery: Examples of the Use of QPatch in Basic Characterization and High Content Screening on Nav, KCa2.3, and Kv11.1 Channels

Journal: Combinatorial Chemistry & High Throughput Screening
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Author(s): Mads P.G. Korsgaard, Dorte Strøbæk and Palle Christophersen

Automated Patch Clamping Using the QPatch

Author(s): Kenneth A. Jones, Nicoletta Garbati, Hong Zhang, and Charles H. Large

Automated Electrophysiology: High Throughput of Art

Author(s): Xiaobo Wang 1), Min Li 2)

Automated and manual patch clamp data of human induced pluripotent stem cell-derived dopaminergic neurons

Author(s): Denise Franz, Hervør Lykke Olsen, Oliver Klink & Jan Gimsa

Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium

Author(s): Ahmed Al-Sabi, Oleg Shamotienko, Sorcha Ni Dhochartaigh, Nagesh Muniyappa, Marie Le Berre, Hamdy Shaban, Jiafu Wang, Jon T. Sack, J. Oliver Dolly

Applying the CiPA approach to evaluate cardiac proarrhythmia risk of some antimalarials used off‐label in the first wave of COVID‐19

Author(s): Annie Delaunois, Matthew Abernathy, Warren D. Anderson, Kylie A. Beattie, Khuram W. Chaudhary, Julie Coulot, Vitalina Gryshkova, Simon Hebeisen, Mark Holbrook, James Kramer, Yuri Kuryshev, Derek Leishman, Isabel Lushbough, Elisa Passini, Will S. Redfern, Blanca Rodriguez, Eric I. Rossman, Cristian Trovato, Caiyun Wu and Jean‐Pierre Valentin

Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria

Author(s): Rolf Hirsch, Jochen Wiesner, Armin Bauer, Alexander Marker, Heiko Vogel, Peter Eugen Hammann and Andreas Vilcinskas

Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria

Author(s): Rolf Hirsch, Jochen Wiesner, Armin Bauer, Alexander Marker, Heiko Vogel, Peter Eugen Hammann and Andreas Vilcinskas

Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of Nav1.7-Mediated Pain

Author(s): Jennifer R. Deuis 1,2, Joshua S. Wingerd 1, Zoltan Winter 3, Thomas Durek 1, Zoltan Dekan 1, Silmara R. Sousa 1, Katharina Zimmermann 3, Tali Hoffmann 3, Christian Weidner 3, Mohammed A. Nassar 4, Paul F. Alewood 1, Richard J. Lewis 1 and Irina Vetter 1,2,*

An Official American Thoracic Society Workshop Report: Translational Research in Rare Respiratory Diseases

Author(s): Kristof AS, Petrof BJ, Hamid Q, Kolb M, Landry JS, MacKenzie A, McCormack FX, Murawski IJ, Moss J, Rauch F, Rosas IO, Shapiro AJ, Smith BM, Thomas DY, Trapnell BC, Young LR, Zariwala MA

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality

Author(s): Christopher R. Butler*† , Kevin Ogilvie§, Luis Martinez-Alsina§, Gabriela Barreiro†, Elizabeth M. Beck†, Charles E. Nolan‡, Kevin Atchison‡, Eric Benvenuti⊥, Leanne Buzon§, Shawn Doran⊥, Cathleen Gonzales‡, Christopher J. Helal§, Xinjun Hou†, Mei-Hui Hsu#, Eric F. Johnson#, Kimberly Lapham⊥, Lorraine Lanyon⊥, Kevin Parris∥, Brian T. O’Neill§, David Riddell‡, Ashley Robshaw‡, Felix Vajdos∥, and Michael A. Brodney†

A spider-venom peptide with multitarget activity on sodium and calcium channels alleviates chronic visceral pain in a model of irritable bowel syndrome

Author(s): Cardoso, Fernanda C., Castro, Joel, Grundy, Luke, Schober, Gudrun, Garcia-Caraballo, Sonia, Zhao, Tianjiao, Herzig, Volker, King, Glenn F., Brierley, Stuart M., Lewis, Richard J.

A Small Molecule Induces Oligodendrogenesis Leading to Myelin Sheath Repair

Journal: Journal of Clinical Endocrinology & Metabolic Disorders
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Author(s): Steven H Nye, James G Yarger

A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo

Author(s): Kristen Frederiksen, Lu Dunguo, Jinhui Yang, Henrik Sindal Jensen, Jesper Frank Bastlund, Peter Hjørringgaard Larsen, Liu Henry, Kim Dekermendjian, Lassina Badolo, Morten Laursen, Charlotte Hougaard, Charles Yang, Niels Svenstrup, Morten Grunnet

A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy

Author(s): Chun Yuen Chow, Yanni K. Y. Chin, LinlinMa, Eivind A. B. Undheim, Volker Herzig, Glenn F. King

A Rational Design of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves that Improves their Impaired Axonal Conduction

Author(s): Ahmed Al-Sabi, Declan Daly, Patrick Hoefer, Gemma K. Kinsella, Charles P. E. Metais, Mark Pickering, Caroline Herron, Seshu Kumar Kaza, Kieran J. Nolan, and J Oliver Dolly

A novel substituted aminoquinoline selectively targets voltage-sensitive sodium channel isoforms and NMDA receptor subtypes and alleviates chronic inflammatory and neuropathic pain

Author(s): Tabakoff B1, Ren W2, Vanderlinden L3, Snell LD4, Matheson CJ5, Wang ZJ6, Levinson R7, Smothers CT8, Woodward JJ9, Honse Y10, Lovinger D11, Rush AM12, Sather WA13, Gustafson DL14, Hoffman PL15.

A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons

Journal: The Journal of Pharmacological and Experimental Therapeutics
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Author(s): Marcelo D. Rosato-Siri, Erika Zambello, Chiara Mutinelli, Nicoletta Garbati, Roberto Benedetti, Laura Aldegheri, Francesca Graziani, Caterina Virginio, Giuseppe Alvaro and Charles H. Large

A novel acetylcholinesterase inhibitor and calcium channel blocker SCR-1693 improves Aβ25–35-impaired mouse cognitive function

Author(s): Zhengping Zhang, Rong Chen, Wenji An, Chunmei Wang, Gaoyong Liao, Xiaoliang Dong, Aijing Bi, Zhimin Yin

A new electro-optical approach for conductance measurement: an assay for the study of drugs acting on ligand-gated ion channels

Author(s): A. Menegon, S. Pitassi, N. Mazzocchi, L. Redaelli, R. Rizzetto, J. F. Rolland, C. Poli, M. Imberti, A. Lanati & F. Grohovaz

A new classifier-based strategy for in-silico ion-channel cardiac drug safety assessment

Author(s): Hitesh B. Mistry 1), Mark R. Davies 2) and Giovanni Y. DiVeroli 3)

A Microscopy-Based Small Molecule Screen in Primary Neurons Reveals Neuroprotective Properties of the FDA-Approved Anti-Viral Drug Elvitegravir

Author(s): Simon F. Merz, C. Peter Bengtson, Clara Tepohl, Anna M. Hagenston, Hilmar Bading & Carlos Bas-Orth

A dipolar cycloaddition reaction to access 6-methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines enables the discovery synthesis and preclinical profiling of a P2X7 antagonist clinical candidate

Author(s): Christa C Chrovian, Akinola Soyode-Johnson, Alexander A Peterson, Christine F. Gelin, Xiaohu Deng, Curt A. Dvorak, Nicholas I. Carruthers, Brian Lord, Ian Fraser, Leah Aluisio, Kevin J Coe, Brian Scott, Tatiana Koudriakova, Freddy Schoetens, Kia Sepassi, David J. Gallacher, Anindya Bhattacharya, and Michael A Letavic

A comprehensive portrait of the venom of the giant red bull ant, Myrmecia gulosa, reveals a hyperdiverse hymenopteran toxin gene family

Author(s): Samuel D. Robinson, Alexander Mueller, Daniel Clayton, Hana Starobova, Brett R. Hamilton, Richard J. Payne, Irina Vetter, Glenn F. King and Eivind A. B. Undheim

A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair

Journal: International journal of Diabetes & Endocrinology
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Author(s): Paula A. Rozenfeld, Daniel Liedtke

A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair

Journal: International journal of Diabetes & Endocrinology
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Author(s): Paual A. Rozenfeld, Daniel Liedtke

4-Substituted carbamazepine derivatives: conformational analysis and sodium channel-blocking properties

Author(s): Yuki Kanase, Takafumi Kitada, Hidetsugu Tabata, Kosho Makino, Tetsuta Oshitari, Hiromi Ohashi, Takashi Yoshinaga, Hideaki Natsugari, Hideyo Takahashi

1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists

Author(s): Fabrizio Micheli*†, Alessia Bacchi§, Simone Braggio†, Laura Castelletti†, Palmina Cavallini†, Paolo Cavanni†, Susanna Cremonesi†, Michele Dal Cin†, Aldo Feriani†, Sylvie Gehanne†, Mahmud Kajbaf†, Luciano Marchió§, Selena Nola†, Beatrice Oliosi†, Annalisa Pellacani†, Elisabetta Perdonà†, Anna Sava†, Teresa Semeraro†, Luca Tarsi†, Silvia Tomelleri†, Andrea Wong†, Filippo Visentini†, Laura Zonzini† and Christian Heidbreder‡