Advancing Ion Channel Research with Automated Patch Clamp (APC) Electrophysiology Platforms
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14.07.2022
Discovery and Evaluation of Novel Angular Fused Pyridoquinazolinonecarboxamides as RNA Polymerase i Inhibitors
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14.07.2022
Environmental levels of carbaryl impair zebrafish larvae behaviour: The potential role of ADRA2B and HTR2B
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14.07.2022
Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines
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28.10.2020
A Microscopy-Based Small Molecule Screen in Primary Neurons Reveals Neuroprotective Properties of the FDA-Approved Anti-Viral Drug Elvitegravir
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28.10.2020
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors
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28.10.2020
Discovery of EST73502, a Dual μ-Opioid Receptor Agonist and σ1 Receptor Antagonist Clinical Candidate for the Treatment of Pain
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28.10.2020
Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency
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28.10.2020
Characterisation of δ-Conotoxin TxVIA as a Mammalian T-Type Calcium Channel Modulator
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28.10.2020
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria
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28.10.2020
Recombinant Production , Bioconjugation and Membrane Binding Studies of Pn3a , a Selective Nav1.7 Inhibitor
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28.10.2020
Discovery, Pharmacological Characterisation and NMR Structure of the Novel µ-Conotoxin SxIIIC, a Potent and Irreversible NaV Channel Inhibitor
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28.10.2020
Cannabidiol Inhibits Multiple Cardiac Ion Channels and Shortens Ventricular Action Potential Duration in Vitro
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28.10.2020
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
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28.10.2020
Inhibitory Effect of Anti-Seizure Medications on Ionotropic Glutamate Receptors: Special Focus on AMPA Receptor Subunits
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28.10.2020
New V1a Receptor Antagonist. Part 2. Identification and Optimization of Triazolobenzazepines
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07.09.2020
Structural optimization of aminopyrimidine-based CXCR4 antagonists
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07.09.2020
Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators
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07.09.2020
Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition
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07.09.2020
A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair
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07.09.2020
Modulation of Lymphocyte Potassium Channel KV1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin
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07.09.2020
Novel bacterial topoisomerase inhibitors derived from isomannide
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07.09.2020
Pharmacological activity and NMR solution structure of the leech peptide HSTX-I
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07.09.2020
Ion Channels and Relevant Drug Screening Approaches
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07.09.2020
Design, Synthesis and Biological Activity of Novel 2,3,4,5-Tetra-Substituted Thiophene Derivatives as PI3Kα Inhibitors with Potent Antitumor Activity
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07.09.2020
Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome
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07.09.2020
Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity
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07.09.2020
Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs
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07.09.2020
Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe
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07.09.2020
Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria
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07.09.2020
Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors
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07.09.2020
Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization
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07.09.2020
Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia
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07.09.2020
A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy
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07.09.2020
Development of a Selective Inhibitor for Kv1.1 Channels Prevalent in Demyelinated Nerves
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21.07.2020
Recombinant production, bioconjugation and membrane binding studies of Pn3a, a selective Nav1.7 inhibitor
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08.07.2020
Structural optimization of aminopyrimidine-based CXCR4 antagonists
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08.07.2020
Screening Technologies for Inward Rectifier Potassium Channels: Discovery of New Blockers and Activators
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08.07.2020
Electrophysiological Studies of GABA-A Receptors Using QPatch II, the Next Generation of Automated Patch‐Clamp Instruments
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08.07.2020
A big Molecule Induces Schwann cells in the peripheral nervous system leading to Myelin Sheath Repair
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08.07.2020
Screening Assay Protocols Targeting the Nav1.7 Channel Using Qube High‐Throughput Automated Patch‐Clamp System
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08.07.2020
Modulation of Lymphocyte Potassium Channel Kv1.3 by Membrane-Penetrating, Joint-Targeting Immunomodulatory Plant Defensin
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08.07.2020
Novel bacterial topoisomerase inhibitors derived from isomannide
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08.07.2020
Pharmacological activity and NMR solution structure of the leech peptide HSTX-I
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08.07.2020
Ion Channels and Relevant Drug Screening Approaches
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08.07.2020
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3Kα inhibitors with potent antitumor activity
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08.07.2020
Privileged scaffold-based design to identify a novel drug-like 5-HT7 receptor-preferring agonist to target Fragile X syndrome
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08.07.2020
Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity
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08.07.2020
Drug-induced QT prolongation: Concordance of preclinical anesthetized canine model in relation to published clinical observations for ten CiPA drugs
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08.07.2020
Characterization of Synthetic Tf2 as a Nav1.3 Selective Pharmacological Probe
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08.07.2020
Antimicrobial Peptides from Rat-Tailed Maggots of the Drone Fly Eristalis tenax Show Potent Activity against Multidrug-Resistant Gram-Negative Bacteria
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08.07.2020
Development of a QPatch-Automated Electrophysiology Assay for Identifying TMEM16A Small-Molecule Inhibitors
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08.07.2020
Fluorescence labeling of a Nav1.7-targeted peptide for near-infrared nerve visualization
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08.07.2020
Inhibition of KCa2 Channels Decreased the Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced Hypokalemia
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08.07.2020
A Selective Nav1.1 Activator with Potential for Treatment of Dravet Syndrome Epilepsy
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08.07.2020
Development of a selective inhibitor for Kv1.1 channels prevalent in demyelinated nerves
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03.06.2020
Mapping the Molecular Surface of the Analgesic Nav1.7-Selective Peptide Pn3a Reveals Residues Essential for Membrane and Channel Interactions
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03.06.2020
Preclinical Safety Assessment of a Highly Selective and Potent Dual Small-Molecule Inhibitor of CBP/P300 in Rats and Dogs
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03.06.2020
Put a cork in it: Plugging the M2 viral ion channel to sink influenza.
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03.06.2020
TMEM16A Potentiation: A Novel Therapeutic Approach for the Treatment of Cystic Fibrosis
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03.06.2020
In vitro characterization of the thermoneutral transient receptor potential vanilloid-1 (TRPV1) inhibitor GRTE16523
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03.06.2020
Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned
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02.06.2020
Manipulation of a spider peptide toxin alters its affinity for lipid bilayers and potency and selectivity for voltage-gated sodium channel subtype
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07.05.2020
A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm
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30.04.2020
Screening assay protocols targeting the Nav1.7 Channel using Qube, a high-throughput automated patch clamp system
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02.04.2020
Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells
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10.02.2020
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
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28.01.2020
Wnts control membrane potential in mammalian cancer cells
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22.01.2020
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
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22.01.2020
Role of High-Throughput Electrophysiology in Drug Discovery
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22.01.2020
Enzymatic Ligation of a Pore Blocker Toxin and a Gating Modifier Toxin: Creating Double-Knotted Peptides with Improved Sodium Channel Nav1.7 Inhibition
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22.01.2020
Venom Peptides with Dual Modulatory Activity on the Voltage-Gated Sodium Channel NaV1.1 Provide Novel Leads for Development of Antiepileptic Drugs
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22.01.2020
Structural optimization of aminopyrimidine-based CXCR4 antagonists
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22.01.2020
Personalized medicine: Vinpocetine to reverse effects of GABRB3 mutation
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22.01.2020
Synthesis and Biological Evaluation of Five‐Atom‐Linker‐Based Arylpiperazine Derivatives with an Atypical Antipsychotic Profile
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22.01.2020
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems
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22.01.2020
Extracellular K+ Dampens T Cell Functions: Implications for Immune Suppression in the Tumor Microenvironment
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23.09.2019
Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain
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23.09.2019
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
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23.09.2019
Development of a high-throughput fluorescent no-wash sodium influx assay
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23.09.2019
From identification to functional characterization of cyriotoxin-1a, an antinociceptive toxin from the spider Cyriopagopus schioedtei.
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23.09.2019
Simultaneous assessment of compound activity on cardiac Nav1.5 peak and late currents in an automated patch clamp platform
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25.04.2019
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
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25.04.2019
Electrophysiological and Pharmacological Characterization of Human Inwardly Rectifying Kir2.1 Channels on an Automated Patch-Clamp Platform
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25.04.2019
Novel Chitohexaose Analog Protects Young and Aged mice from CLP Induced Polymicrobial Sepsis
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25.04.2019
Drug Repurposing: The Anthelmintics Niclosamide and Nitazoxanide are Potent TMEM16A Antagonists that Fully Bronchodilate Airway
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25.04.2019
Differential Free Intracellular Calcium Release by Class II Antiarrhythmics in Cancer Cell Lines
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25.04.2019
Benzothiophenes as Potent Analgesics Against Neuropathic Pain
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25.04.2019
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
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25.04.2019
Synthesis of Pseudellone Analogs and Characterization as Novel T-type Calcium Channel Blockers
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03.01.2019
Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel
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03.01.2019
Biological Profiling of Coleoptericins and Coleoptericin-Like Antimicrobial Peptides from the Invasive Harlequin Ladybird Harmonia axyridis
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03.01.2019
Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain
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13.12.2018
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis
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08.10.2018
Selective Nav1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain
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08.10.2018
Inhibitory effects of cannabidiol on voltage-dependent sodium currents
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19.09.2018
A comprehensive portrait of the venom of the giant red bull ant, Myrmecia gulosa, reveals a hyperdiverse hymenopteran toxin gene family
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19.09.2018
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.
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19.09.2018
Screening strategies for the discovery of ion channel monoclonal antibodies
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19.09.2018
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
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05.07.2018
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect
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05.07.2018
GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability
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05.07.2018
The E15R Point Mutation in Scorpion Toxin Cn2 Uncouples Its Depressant and Excitatory Activities on Human NaV1.6
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05.07.2018
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy
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05.07.2018
Direct evidence for high affinity blockade of NaV1.6 channel subtype by huwentoxin-IV spider peptide, using multiscale functional approaches
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15.05.2018
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
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11.04.2018
4-Substituted carbamazepine derivatives: conformational analysis and sodium channel-blocking properties
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23.03.2018
Identification of Selective Inhibitors of the Potassium Channel Kv1.1–1.2(3) by High-Throughput Virtual Screening and Automated Patch Clamp
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02.03.2018
A Small Molecule Induces Oligodendrogenesis Leading to Myelin Sheath Repair
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30.01.2018
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
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13.12.2017
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
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11.12.2017
Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells: An In-Vitro Model to Predict Cardiac Effects of Drugs
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09.11.2017
The sodium channel activator Lu AE98134 normalizes the altered firing properties of fast spiking interneurons in Dlx5/6+/− mice
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09.11.2017
Eleclazine exhibits enhanced selectivity for long QT syndrome type 3–associated late Na+ current
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09.11.2017
Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K+ Channels in Pigs
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09.11.2017
Cardiac sodium channel antagonism – Translation of preclinical in vitro assays to clinical QRS prolongation
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07.11.2017
Discovery and electrophysiological characterization of SKF-32802; a novel hERG agonist found through a large-scale structural similarity search
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27.09.2017
Clathrodin, hymenidin and oroidin, and their synthetic analogues as inhibitors of the voltage-gated potassium channels
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27.09.2017
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
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27.09.2017
Discovery and mode of action of a novel analgesic β-toxin from the African spider Ceratogyrus darlingi
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27.09.2017
Pharmacological screening technologies for venom peptide discovery
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27.09.2017
Biphenyloxy-alkyl-piperidine and azepane derivatives as histamine H3 receptor ligands
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27.09.2017
An Official American Thoracic Society Workshop Report: Translational Research in Rare Respiratory Diseases
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27.09.2017
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
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15.08.2017
Using automated patch clamp electrophysiology platforms in pain-related ion channel research: insights from industry and academia
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29.06.2017
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
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02.06.2017
Effect of antiarrhythmic drugs on small conductance calcium – activated potassium channels
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17.05.2017
Intracellular Calcium Mobilization in Response to Ion Channel Regulators via a Calcium-Induced Calcium Release Mechanism
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02.05.2017
NS19504: a novel BK channel activator with relaxing effect on bladder smooth muscle spontaneous phasic contractions
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28.04.2017
Development of Automated Patch Clamp Technique to Investigate CFTR Chloride Channel Function
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27.04.2017
Calcium-activated chloride channel ANO1 promotes breast cancer progression by activating EGFR and CAMK signaling
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25.04.2017
Automated and manual patch clamp data of human induced pluripotent stem cell-derived dopaminergic neurons
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11.04.2017
Arrangement of Kv1 α subunits dictates sensitivity to tetraethylammonium
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04.04.2017
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
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04.04.2017
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
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04.04.2017
High throughput physiological screening of iPSC-derived cardiomyocytes for drug development
