SYNTHESIS OF CONFORMATIONALLY-CONSTRAINED STEREOSPECIFIC ANALOGS OF GLUTAMIC-ACID AS ANTAGONISTS OF METABOTROPIC RECEPTORS

被引:19
作者
TELLIER, F
ACHER, F
BRABET, I
PIN, JP
BOCKAERT, J
AZERAD, R
机构
[1] UNIV PARIS 05,CHIM & BIOCHIM PHARMACOL & TOXICOL LAB,CNRS,U400,F-75270 PARIS 06,FRANCE
[2] CNRS,INSERM,CTR PHARMACOL ENDOCRINOL,UPR 9023,F-34094 MONTPELLIER 5,FRANCE
关键词
D O I
10.1016/0960-894X(95)00457-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Rigid analogs of ACPD have been synthesized to mimick different potential conformations of ACPD in aqueous solution. One of them, (+/-)-ABHD-I is a competitive antagonist at mGluR1a receptor with a K-B value of 300 mu M.
引用
收藏
页码:2627 / 2632
页数:6
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