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

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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-D-aspartate (NMDA) receptor. In vitro receptor binding using [3H]-L-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 [3H]kainate binding to assess selectivity over non-NMDA glutamate receptors. Of the compounds tested, 4,5-methano-AP5 analogue 26 was the most potent selective NMDA antagonist; however, potency was lower than that for [[(+/-)-2-carboxypiperidin-4-yl]methyl]phosphonic acid (CGS 19755, 5).

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