Literature DB >> 12852750

(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.

Yong-Jin Wu1, Christopher G Boissard, Corinne Greco, Valentin K Gribkoff, David G Harden, Huan He, Alexandre L'Heureux, Shing Hong Kang, Gene G Kinney, Ronald J Knox, Joanne Natale, Amy E Newton, Sanna Lehtinen-Oboma, Michael W Sinz, Digavalli V Sivarao, John E Starrett, Li-Qiang Sun, Svetlana Tertyshnikova, Mark W Thompson, David Weaver, Henry S Wong, Lei Zhang, Steven I Dworetzky.   

Abstract

(S)-N-[1-(3-Morpholin-4-ylphenyl)ethyl]-3-phenylacrylamide (2) was synthesized as an orally bioavailable KCNQ2 potassium channel opener. In a rat model of migraine, 2 demonstrated significant oral activity in reducing the total number of cortical spreading depressions induced by potassium chloride.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 12852750     DOI： 10.1021/jm034073f

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 in total

Review 1.  K+ channel modulators for the treatment of neurological disorders and autoimmune diseases.

Authors:  Heike Wulff; Boris S Zhorov
Journal:  Chem Rev       Date:  2008-05       Impact factor: 60.622

2.  From pan-reactive KV7 channel opener to subtype selective opener/inhibitor by addition of a methyl group.

Authors:  Sigrid Marie Blom; Mario Rottländer; Jan Kehler; Christoffer Bundgaard; Nicole Schmitt; Henrik Sindal Jensen
Journal:  PLoS One       Date:  2014-06-23       Impact factor: 3.240

Review 3.  Migraine is a neuronal disease.

Authors:  J Tajti; A Párdutz; E Vámos; B Tuka; A Kuris; Zs Bohár; A Fejes; J Toldi; L Vécsei
Journal:  J Neural Transm (Vienna)       Date:  2010-12-15       Impact factor: 3.575

4.  Oxidation mechanism in the metabolism of (S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]-3-phenylacrylamide on oxyferryl active site in CYP3A4 Cytochrome: DFT modeling.

Authors:  Abdul Rajjak Shaikh; Ewa Broclawik; Hideyuki Tsuboi; Michihisa Koyama; Akira Endou; Hiromitsu Takaba; Momoji Kubo; Carlos A Del Carpio; Akira Miyamoto
Journal:  J Mol Model       Date:  2007-03-27       Impact factor: 1.810

5.  Cortical spreading depression-new insights and persistent questions.

Authors:  A Charles; Kc Brennan
Journal:  Cephalalgia       Date:  2009-10       Impact factor: 6.292

6.  The impact of anesthetics and hyperoxia on cortical spreading depression.

Authors:  Chiho Kudo; Ala Nozari; Michael A Moskowitz; Cenk Ayata
Journal:  Exp Neurol       Date:  2008-04-11       Impact factor: 5.330

Review 7.  Cortical spreading depression: culprits and mechanisms.

Authors:  Aparna Ann Mathew; Rajitha Panonnummal
Journal:  Exp Brain Res       Date:  2022-01-22       Impact factor: 1.972

Review 8.  Chemical modulation of Kv7 potassium channels.

Authors:  Matteo Borgini; Pravat Mondal; Ruiting Liu; Peter Wipf
Journal:  RSC Med Chem       Date:  2021-01-14

9.  Activation of Kv7 Potassium Channels Inhibits Intracellular Ca2+ Increases Triggered By TRPV1-Mediated Pain-Inducing Stimuli in F11 Immortalized Sensory Neurons.

Authors:  Paolo Ambrosino; Maria Virginia Soldovieri; Erika Di Zazzo; Gianluca Paventi; Fabio Arturo Iannotti; Ilaria Mosca; Francesco Miceli; Cristina Franco; Lorella Maria Teresa Canzoniero; Maurizio Taglialatela
Journal:  Int J Mol Sci       Date:  2019-09-04       Impact factor: 5.923

10.  Persistent sodium current blockers can suppress seizures caused by loss of low-threshold D-type potassium currents: Predictions from an in silico study of Kv1 channel disorders.

Authors:  Jiaxin Du; Viktor Vegh; David C Reutens
Journal:  Epilepsia Open       Date:  2020-01-22
  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.