N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.
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.
Hu
L Y
LY
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Ryder
T R
TR
Rafferty
M F
MF
Cody
W L
WL
Lotarski
S M
SM
Miljanich
G P
GP
Millerman
E
E
Rock
D M
DM
Song
Y
Y
Stoehr
S J
SJ
Taylor
C P
CP
Weber
M L
ML
Szoke
B G
BG
Vartanian
M G
MG
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
D002121:Calcium Channel Blockers; D003959:Diamines; D004151:Dipeptides