Neuronal N-type calcium channel blockers: a series of 4-piperidinylaniline analogs with analgesic activity.
Several novel N-type voltage sensitive calcium channel blockers showed high affinity in the IMR32 assay and efficacy in the anti-writhing model. Herein, we describe the design, synthesis, SAR studies, biological data, physicochemical properties and pharmacokinetics of this 4-piperidinylaniline series.
Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
L Y
LY
Hu
T R
TR
Ryder
M F
MF
Rafferty
K M
KM
Siebers
T
T
Malone
A
A
Chatterjee
M R
MR
Feng
S M
SM
Lotarski
D M
DM
Rock
S J
SJ
Stoehr
C P
CP
Taylor
M L
ML
Weber
G P
GP
Miljanich
E
E
Millerman
B G
BG
Szoke
D018712:Analgesics, Non-Narcotic / Q000494:pharmacology*; D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis / Q000494:pharmacology*; D020864:Calcium Channels, N-Type / Q000187:drug effects*; D051379:Mice; D013329:Structure-Activity Relationship
D018712:Analgesics, Non-Narcotic; D000814:Aniline Compounds; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type