Neuronal N-type calcium channel blockers: a series of 4-piperidinylaniline analogs with analgesic activity

Authors :: L Y, Hu
T R, Ryder
M F, Rafferty
K M, Siebers
T, Malone
A, Chatterjee
M R, Feng
S M, Lotarski
D M, Rock
S J, Stoehr
C P, Taylor
M L, Weber
G P, Miljanich
E, Millerman
B G, Szoke
Source :: Drug design and discovery. 17(1)
Publication Year :: 2000
Abstract: 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.

Subjects :: Mice
Structure-Activity Relationship
Aniline Compounds
Calcium Channels, N-Type
Animals
Analgesics, Non-Narcotic
Calcium Channel Blockers

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