title: A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.
abstract: N-type calcium channels (Ca(v)2.2) have been shown to play a critical role in pain. A series of low molecular weight 2-aryl indoles were identified as potent Ca(v)2.2 blockers with good in vitro and in vivo potency.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. sriram_tyagarajan@merck.com
authors.forename: Sriram
authors.initials: S
authors.lastname: Tyagarajan
authors.forename: Prasun K
authors.initials: PK
authors.lastname: Chakravarty
authors.forename: Min
authors.initials: M
authors.lastname: Park
authors.forename: Bishan
authors.initials: B
authors.lastname: Zhou
authors.forename: James B
authors.initials: JB
authors.lastname: Herrington
authors.forename: Kevin
authors.initials: K
authors.lastname: Ratliff
authors.forename: Randall M
authors.initials: RM
authors.lastname: Bugianesi
authors.forename: Brande
authors.initials: B
authors.lastname: Williams
authors.forename: Rodolfo J
authors.initials: RJ
authors.lastname: Haedo
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Swensen
authors.forename: Vivien A
authors.initials: VA
authors.lastname: Warren
authors.forename: McHardy
authors.initials: M
authors.lastname: Smith
authors.forename: Maria
authors.initials: M
authors.lastname: Garcia
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Kaczorowski
authors.forename: Owen B
authors.initials: OB
authors.lastname: McManus
authors.forename: Kathryn A
authors.initials: KA
authors.lastname: Lyons
authors.forename: Xiaohua
authors.initials: X
authors.lastname: Li
authors.forename: Maria
authors.initials: M
authors.lastname: Madeira
authors.forename: Bindhu
authors.initials: B
authors.lastname: Karanam
authors.forename: Mitchell
authors.initials: M
authors.lastname: Green
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Forrest
authors.forename: Catherine
authors.initials: C
authors.lastname: Abbadie
authors.forename: Erin
authors.initials: E
authors.lastname: McGowan
authors.forename: Shruti
authors.initials: S
authors.lastname: Mistry
authors.forename: Nina
authors.initials: N
authors.lastname: Jochnowitz
authors.forename: Joseph L
authors.initials: JL
authors.lastname: Duffy
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D020864:Calcium Channels, N-Type / Q000378:metabolism*; D004285:Dogs; D000882:Haplorhini; D006801:Humans; D007211:Indoles / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D010146:Pain / Q000188:drug therapy*; D051381:Rats
chemical_list: C500545:CACNA1B protein, human; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D007211:Indoles