title: Imidazopyridines: a novel class of hNav1.7 channel blockers.
abstract: A series of imidazopyridines were evaluated as potential sodium channel blockers for the treatment of neuropathic pain. Several members were identified with good hNa(v)1.7 potency and excellent rat pharmacokinetic profiles. Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. clare_london@merck.com
authors.forename: Clare
authors.initials: C
authors.lastname: London
authors.forename: Scott B
authors.initials: SB
authors.lastname: Hoyt
authors.forename: William H
authors.initials: WH
authors.lastname: Parsons
authors.forename: Brande S
authors.initials: BS
authors.lastname: Williams
authors.forename: Vivien A
authors.initials: VA
authors.lastname: Warren
authors.forename: Richard
authors.initials: R
authors.lastname: Tschirret-Guth
authors.forename: McHardy M
authors.initials: MM
authors.lastname: Smith
authors.forename: Birgit T
authors.initials: BT
authors.lastname: Priest
authors.forename: Erin
authors.initials: E
authors.lastname: McGowan
authors.forename: William J
authors.initials: WJ
authors.lastname: Martin
authors.forename: Kathryn A
authors.initials: KA
authors.lastname: Lyons
authors.forename: Xiaohua
authors.initials: X
authors.lastname: Li
authors.forename: Bindhu V
authors.initials: BV
authors.lastname: Karanam
authors.forename: Nina
authors.initials: N
authors.lastname: Jochnowitz
authors.forename: Maria L
authors.initials: ML
authors.lastname: Garcia
authors.forename: John P
authors.initials: JP
authors.lastname: Felix
authors.forename: Brian
authors.initials: B
authors.lastname: Dean
authors.forename: Catherine
authors.initials: C
authors.lastname: Abbadie
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Kaczorowski
authors.forename: Joseph L
authors.initials: JL
authors.lastname: Duffy
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D007249:Inflammation / Q000188:drug therapy; D015394:Molecular Structure; D062556:NAV1.7 Voltage-Gated Sodium Channel; D010146:Pain / Q000188:drug therapy; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D026941:Sodium Channel Blockers / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D015222:Sodium Channels / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D062556:NAV1.7 Voltage-Gated Sodium Channel; D011725:Pyridines; C486866:SCN9A protein, human; D026941:Sodium Channel Blockers; D015222:Sodium Channels