ZAPA，（Z）-3-[(氨基亚氨甲基)硫代]-2-丙烯盐酸盐，一种对蛔虫肌细胞上GABA受体有强效激动作用的物质。
ZAPA, (Z)-3-[(aminoiminomethyl)thio]-2-propenoic acid hydrochloride, a potent agonist at GABA-receptors on the Ascaris muscle cell.
作者信息
Holden-Dye L, Walker R J
机构信息
Department of Neurophysiology, University of Southampton.
出版信息
Br J Pharmacol. 1988 Sep;95(1):3-5. doi: 10.1111/j.1476-5381.1988.tb16540.x.
Abstract
This study is the first report of a compound which is equal in efficacy to gamma-aminobutyric acid (GABA) at the nematode Ascaris muscle GABA-receptor. The GABA-receptor at the Ascaris muscle cell which mediates a membrane hyperpolarization and muscle relaxation has eluded classification. The structure-activity profile of this receptor is not typical of GABAA or GABAB-receptors. Here we report that the isothiouronium compound ZAPA is as potent as GABA at this receptor. This finding has important implications for the characterization of the Ascaris GABA-receptor and the design of novel anthelmintics.
摘要
本研究首次报道了一种化合物，其在蛔虫肌肉γ-氨基丁酸（GABA）受体上的功效与GABA相当。蛔虫肌肉细胞上介导膜超极化和肌肉松弛的GABA受体一直未得到分类。该受体的构效关系并不具有典型的GABAA或GABAB受体特征。在此我们报道，异硫脲化合物ZAPA在该受体上与GABA具有同等效力。这一发现对于蛔虫GABA受体的特性表征以及新型驱虫药的设计具有重要意义。
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