title: Discovery and SAR of novel tetrahydropyrrolo[3,4-c]pyrazoles as inhibitors of the N-type calcium channel.
abstract: A novel series of substituted tetrahydropyrrolo[3,4-c]pyrazoles were investigated as blockers of the N-type calcium channel (Cav2.2 channels), a chronic pain target.
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA. Electronic address: mwinter4@its.jnj.com.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Winters
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Nalin
authors.initials: N
authors.lastname: Subasinghe
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Mark
authors.initials: M
authors.lastname: Wall
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Edward
authors.initials: E
authors.lastname: Beck
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Michael R
authors.initials: MR
authors.lastname: Brandt
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Michael F A
authors.initials: MF
authors.lastname: Finley
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Yi
authors.initials: Y
authors.lastname: Liu
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Mary Lou
authors.initials: ML
authors.lastname: Lubin
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Neeper
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Ning
authors.initials: N
authors.lastname: Qin
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Flores
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D020864:Calcium Channels, N-Type / Q000378:metabolism*; D059350:Chronic Pain / Q000188:drug therapy; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D011720:Pyrazoles / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: C500545:CACNA1B protein, human; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D011720:Pyrazoles
keywords: Ca(v)2.2 blockers; N-type calcium channel; Pain; Tetrahydropyrrolo[3,4-c]pyrazoles