Title of article :
(2S,4S)-2-Amino-4-(2,2-diphenylethyl)pentanedioic acid selective group 2 metabotropic glutamate receptor antagonist
Author/Authors :
Ana Escribano، نويسنده , , Jesus Ezquerra، نويسنده , , Concepci?n Pedregal، نويسنده , , Almudena Rubio، نويسنده , , Belén Yruretagoyena، نويسنده , , S. Richard Baker، نويسنده , , Rebecca A. Wright، نويسنده , , Bryan G. Johnson، نويسنده , , Darryle D. Schoepp، نويسنده ,
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 a 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.
