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(2S,4S)-amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist.

作者信息

Escribano A, Ezquerra J, Pedregal C, Rubio A, Yruretagoyena B, Baker S R, Wright R A, Johnson B G, Schoepp D D

机构信息

Centro de Investigación Lilly, Madrid, Spain.

出版信息

Bioorg Med Chem Lett. 1998 Apr 7;8(7):765-70. doi: 10.1016/s0960-894x(98)00091-2.

DOI:10.1016/s0960-894x(98)00091-2
PMID:9871538
Abstract

(2S,4S)-2-Amino-4-(4,4-diphenylbut-1-yl)-pentane-1,5-dioic acid 1m, is a novel metabotropic glutamate receptor (mGluR) antagonist with insignificant ionotropic affinity. It is selective antagonist of negatively-coupled cAMP-linked mGluRs with no effect on phosphoinositide coupled mGluRs. A series of 4-substituted glutamic acid analogues were prepared and it was found that compound 1k is tenfold more potent than 1m. Compound 1k has neither significant affinity for ionotropic glutamate receptors nor group 1 and 3 metabotropic receptors.

摘要

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