γ-Aminobutyric Acid Uptake Inhibition and Anticonvulsant Activity of Nipecotic Acid Esters
作者:A. Michael Crider、J.D. Wood、Kathryn D. Tschappat、Christine N. Hinko、Karen Seibert
DOI:10.1002/jps.2600731132
日期:1984.11
n-Alkyl esters of nipecotic acid were prepared by Fischer esterification, and the esters were evaluated against bicuculline-induced seizures in mice. Evaluation of the alkyl esters for inhibition of gamma-aminobutyric acid uptake into mouse whole brain mini-slices revealed that the order of potency was proportional to chain length. The octyl ester inhibited gamma-aminobutyric acid and beta-alanine
通过Fischer酯化反应制备了庚酸的正烷基酯,并评估了该酯类对双瓜氨酸诱导的小鼠癫痫发作的作用。烷基酯对小鼠全脑小切片中γ-氨基丁酸摄取抑制作用的评估显示,效价的顺序与链长成正比。辛酯通过明显的非特异性机制抑制了γ-氨基丁酸和β-丙氨酸的摄取。还使用二环己基碳二亚胺或1,1'-羰基二咪唑作为缩合剂,合成了多种乳酸菌的苯基酯。大多数苯基酯是γ-氨基丁酸摄取的有效抑制剂。摄取抑制似乎涉及特异性和非特异性(类似洗涤剂的)机制。