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,*

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

Author(s): Damian Bell, Mark Dallas

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 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.

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 a, b, Lei Huang a, b, Qingwei Zhang a, b, Jianqi Li a

Study of TRP Channels by Automated Patch Clamp Systems

Author(s): Morten Sunesen, Rasmus B Jacobsen

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

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

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)

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

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

Author(s): Jennifer R. Deuis 1), Zoltan Dekan 1), Joshua S. Wingerd 1), Jennifer J. Smith 1), Nehan R. Munasinghe 2), Rebecca F. Bhola 2), Wendy L. Imlach 2), Volker Herzig 1), David A. Armstrong 3), K. Johan Rosengren 3), Frank Bosmans 4), Stephen G. Waxman 5), Sulayman D. Dib-Hajj 5), Pierre Escoubas 6), Michael S. Minett 7), Macdonald J. Christie 2), Glenn F. King 1), Paul F. Alewood 1), Richard J. Lewis 1), John N. Wood 7) & Irina Vetter 1,8)

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

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

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.

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‡

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

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 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

Journal: Scientific Reports 7, Article number: 39662 (2017)
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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

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

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

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)

GABA-A a17B3y2 on QPatch

Author(s): Hervor L Olsen, M Knirke Jensen

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)

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*

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

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 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

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 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)

Developing Molecular Pharmacology of BK Channels for Therapeutic Benefit

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

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 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

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.

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

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)

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)

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

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

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

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

Journal: Journal of Medicinal Chemistry DOI: 10.1021/acs.jmedchem.6b01262
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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

Journal: Scientific Reports 7, Article number: 44843 (2017)
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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)

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‡

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