Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Research Abstract Details 

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Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Abstract Text:

Scott B Hoyt,Clare London,David Gorin,Matthew J Wyvratt,Michael H Fisher,Catherine Abbadie,John P Felix,Maria L Garcia,Xiaohua Li,Kathryn A Lyons,Erin McGowan,D Euan MacIntyre,William J Martin,Birgit T Priest,Amy Ritter,McHardy M Smith,Vivien A Warren,Brande S Williams,Gregory J Kaczorowski,William H Parsons,

A series of benzodiazepines and benzazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of the benzazepinone series, compound 47, displayed potent, state-dependent block of hNa(v)1.7, and was orally efficacious in a rat model of neuropathic pain.

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Publishing Authors By Initials

SB Hoyt,C London,D Gorin,MJ Wyvratt,MH Fisher,C Abbadie,JP Felix,ML Garcia,X Li,KA Lyons,E McGowan,DE MacIntyre,WJ Martin,BT Priest,A Ritter,MM Smith,VA Warren,BS Williams,GJ Kaczorowski,WH Parsons,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 4630-4

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 27

MONTH: 05

YEAR: 2007

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: metabolism

Chemical & Substance for Abstract: Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain. Information

Substance Name: Sodium Channels

Registry Number: 0

Grant and Affiliation Information for Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.

AFFILIATION: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. scott_hoyt@merck.com

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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