31 articles for thisTarget
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Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.
University of Kansas Specialized Chemistry Center
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.
Bristol-Myers Squibb
(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.
Vanderbilt University Medical Center
3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.
Astrazeneca
Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator.
Vanderbilt University Medical Center
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Bristol-Myers Squibb Pharmaceutical Research Institute
Advances in Epilepsy: Mechanisms, Clinical Trials, and Drug Therapies.
Sichuan University
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.
Shanghai Institute of Materia Medica
Discovery, synthesis and biological characterization of a series of
University of Nebraska
Development of an automated screen for Kv7.2 potassium channels and discovery of a new agonist chemotype.
University of Michigan
(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.
Bristol-Myers Squibb Pharmaceutical Research Institute
The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.
The Bristol-Myers Squibb Pharmaceutical Research Institute
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
Bristol-Myers Squibb Pharmaceutical Research Institute
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.
Marquette University
Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.
University Federico Ii of Naples
Discovery of Novel Retigabine Derivatives as Potent KCNQ4 and KCNQ5 Channel Agonists with Improved Specificity.
Chinese Academy of Sciences
Design, synthesis and evaluation of novel N-phenylbutanamide derivatives as KCNQ openers for the treatment of epilepsy.
Nanjing University of Technology
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.
Nanjing University of Technology
TRIAZINE DERIVATIVES FOR THE TREATMENT OF TUMOURS AND NEURODEGENERATIVE DISORDERS
UNIVERSITA'' DEGLI STUDI DI MILANO
COMPOUNDS AND THE USES AND PHARMACEUTICAL COMPOSITIONS THEREOF
Beijing Youzhuju Network Technology Co.