Synthesis and biological evaluation of cyclopropyl analogs of 2-amino-5-phosphonopentanoic acid

…, R Pellicciari, B Natalini, JB Monahan…

Index: Dappen, Michael S.; Pellicciari, Roberto; Natalini, Benedetto; Monahan, Joseph B.; Chiorri, Claudio; Cordi, Alex A. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 161 - 168

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Citation Number: 51

Abstract

A series of cyclopropyl analogues related to 2-amino-5-phosphonopentanoic acid (AP5) were synthesized and their biological activity was assessed as competitive antagonists for the N-methyl-Baspartate (NMDA) receptor. In vitro receptor binding using [SH]-~-glutamate as the radioligand provided affinity data, while modulation of [3H] MK-801 binding was used as a functional assay. The analogues were also evaluated in [%] kainate binding to ...