title: Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
abstract: A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
authors: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. scott_hoyt@merck.com
authors: Scott B
authors: SB
authors: Hoyt
authors: Clare
authors: C
authors: London
authors: Hyun
authors: H
authors: Ok
authors: Edward
authors: E
authors: Gonzalez
authors: Joseph L
authors: JL
authors: Duffy
authors: Catherine
authors: C
authors: Abbadie
authors: Brian
authors: B
authors: Dean
authors: John P
authors: JP
authors: Felix
authors: Maria L
authors: ML
authors: Garcia
authors: Nina
authors: N
authors: Jochnowitz
authors: Bindhu V
authors: BV
authors: Karanam
authors: Xiaohua
authors: X
authors: Li
authors: Kathryn A
authors: KA
authors: Lyons
authors: Erin
authors: E
authors: McGowan
authors: D Euan
authors: DE
authors: Macintyre
authors: William J
authors: WJ
authors: Martin
authors: Birgit T
authors: BT
authors: Priest
authors: McHardy M
authors: MM
authors: Smith
authors: Richard
authors: R
authors: Tschirret-Guth
authors: Vivien A
authors: VA
authors: Warren
authors: Brande S
authors: BS
authors: Williams
authors: Gregory J
authors: GJ
authors: Kaczorowski
authors: William H
authors: WH
authors: Parsons
mesh_terms: D000818:Animals; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001682:Biological Availability; D004195:Disease Models, Animal; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D015394:Molecular Structure; D062556:NAV1.7 Voltage-Gated Sodium Channel; D009437:Neuralgia / Q000188:drug therapy*; D051381:Rats; D026941:Sodium Channel Blockers / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015222:Sodium Channels / Q000737:chemistry / Q000187:drug effects*
chemical_list: D001570:Benzodiazepinones; D062556:NAV1.7 Voltage-Gated Sodium Channel; C503480:Scn9a protein, rat; D026941:Sodium Channel Blockers; D015222:Sodium Channels