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

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

Drug design and discovery（2000）

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摘要

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.

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关键词

analgesic activity,calcium,n-type

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