(2S,4S)-2-AMINO-4-(2,2-DIPHENYLETHYL) PENTANEDIOIC ACID SELECTIVE GROUP 2 METABOTROPIC GLUTAMATE-RECEPTOR ANTAGONIST

Authors
ESCRIBANO A EZQUERRA J PEDREGAL C RUBIO A YRURETAGOYENA B BAKER SR WRIGHT RA JOHNSON BG SCHOEPP DD
Citation
A. Escribano et al., (2S,4S)-2-AMINO-4-(2,2-DIPHENYLETHYL) PENTANEDIOIC ACID SELECTIVE GROUP 2 METABOTROPIC GLUTAMATE-RECEPTOR ANTAGONIST, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 765-770
Citations number
12
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
7
Year of publication
1998
Pages
765 - 770
Database
ISI
SICI code
0960-894X(1998)8:7<765:(PASG>2.0.ZU;2-5
Abstract
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 a selective antagonist of negatively-coupl ed cAMP-linked mGluRs with no effect on phosphoinositide coupled mGluR s. A series of 4-substituted glutamic acid analogues were prepared and it was found that compound 1k is tenfold more potent than 1m. Compoun d 1k has neither significant affinity for ionotropic glutamate recepto rs nor group 1 and 3 metabotropic receptors. (C) 1998 Elsevier Science Ltd. All rights reserved.