Design and Synthesis of Photoaffinity Probe Candidates for the GABA-gated Chloride Channel

作     者：刘尚钟 LI Qing-X. 

作者机构：Department of Applied Chemistry China Agricultural University Beijing 100094 China Department of Molecular Biosciences and Bioengineering University of Hawaii at Manoa Honolulu Hawaii 96822 USA 

基　　金：the National Basic Research Program of China(2003CB 114405) Hawaii Heptachlor Education, Research Foundation,USDA-ARS award number 58-5320-3-315 

出 版 物：《Chinese Journal of Chemistry》 (中国化学（英文版）)

年 卷 期：2006年第24卷第10期

页      码：1435-1438页

摘      要：In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel, new photoaffinity probe candidates based on 5e-t-butyl-2e-[4-（substituted-propynyl）phenyl]-1,3-dithiane for the noncompetitive blocker （NCB） site of the γ-aminobutyric acid （GABA）-gated chloride channel were designed and synthesized, and their potency as an inhibitor on NCB was measured by 4＇-ethynyl-4-n-[2,3-^3H2]-propylbicycloorthobenzoate （^3H EBOB） assay. The synthesized compounds showed high inhibition activities with half maximum inhibition concentrations （IC50） of lower than 35 nmol/L and were very stable in binding conditions as well photoreacted quickly at 300 nm light. These new compounds are expected to be good photoaffinity labeling probes if radioisotope iodine is incorporated.

主 题 词：photoaffinity labeling GABA receptor 1,3-dithiane 

学科分类：081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 070303[070303] 0703[理学-化学类] 

核心收录：

D　O　I：10.1002/cjoc.200690269

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