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.
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
Siebers
K M
KM
Malone
T
T
Chatterjee
A
A
Feng
M R
MR
Lotarski
S M
SM
Rock
D M
DM
Stoehr
S J
SJ
Taylor
C P
CP
Weber
M L
ML
Miljanich
G P
GP
Millerman
E
E
Szoke
B G
BG
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