title: N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.
abstract: Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.
authors: Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
authors: L Y
authors: LY
authors: Hu
authors: T R
authors: TR
authors: Ryder
authors: M F
authors: MF
authors: Rafferty
authors: W L
authors: WL
authors: Cody
authors: S M
authors: SM
authors: Lotarski
authors: G P
authors: GP
authors: Miljanich
authors: E
authors: E
authors: Millerman
authors: D M
authors: DM
authors: Rock
authors: Y
authors: Y
authors: Song
authors: S J
authors: SJ
authors: Stoehr
authors: C P
authors: CP
authors: Taylor
authors: M L
authors: ML
authors: Weber
authors: B G
authors: BG
authors: Szoke
authors: M G
authors: MG
authors: Vartanian
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis*; D003959:Diamines / Q000138:chemical synthesis* / Q000494:pharmacology*; D004151:Dipeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D004195:Disease Models, Animal; D051379:Mice; D008811:Mice, Inbred DBA; D008956:Models, Chemical; D012640:Seizures / Q000188:drug therapy
chemical_list: D002121:Calcium Channel Blockers; D003959:Diamines; D004151:Dipeptides