神经元n型钙通道阻滞剂:一系列具有镇痛活性的4-哌啶苯胺类似物。

Drug design and discovery Pub Date : 2000-01-01

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

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引用次数: 0

摘要

几种新型n型电压敏感钙通道阻滞剂在IMR32实验中显示出高亲和力，在抗扭体模型中显示出有效。本文介绍了该4-哌啶苯胺系列的设计、合成、SAR研究、生物学数据、理化性质和药代动力学。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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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.

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Drug design and discovery

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