N,N-二烷基二肽基胺作为N型钙通道阻滞剂系列中亮氨酸侧链的构效关系

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

T R Ryder, L Y Hu, M F Rafferty, 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

对一系列N,N-二烷基二肽胺在N型VSCC中具有有效功能活性的亮氨酸侧链周围的SAR进行了探索。公开了一种新的类似物，其具有改进的水溶性，在听源性癫痫模型中具有体内活性，并且在电生理测定中具有可逆阻断。

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Structure-activity relationship at the leucine side chain in a series of N,N-dialkyldipeptidyl-amines as N-type calcium channel blockers.

Exploration of the SAR around the leucine side chain in a series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC is presented. A novel analog is disclosed which possesses improved aqueous solubility, in vivo activity in an audiogenic seizure model, and reversible blockade in electrophysiological assays.

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Drug design and discovery

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