基于肽药效团模型设计高亲和力拟肽类阿片激动剂。
Design of a high affinity peptidomimetic opioid agonist from peptide pharmacophore models.
作者信息
Wang C, McFadyen I J, Traynor J R, Mosberg H I
机构信息
College of Pharmacy, University of Michigan, Ann Arbor 48109, USA.
出版信息
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2685-8. doi: 10.1016/s0960-894x(98)00472-7.
PMID:9873603
Abstract
A pair of diastereomeric peptidomimetics based upon opioid receptor-binding pharmacophore models derived for a series of opioid tetrapeptides was synthesized. Both analogues display high opioid receptor affinity, moderate selectivity for the mu opioid receptor, and are potent, full agonists.
摘要
基于从一系列阿片类四肽衍生的阿片受体结合药效团模型合成了一对非对映异构的拟肽。两种类似物均显示出高阿片受体亲和力、对μ阿片受体的适度选择性，并且是强效的完全激动剂。
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