Document Report Card

ID: ALA1122476

Journal: J Med Chem

Title: Enzymic resolution and binding to rat brain membranes of the glutamic acid agonist alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid.

Authors: Hansen JJ, Lauridsen J, Nielsen E, Krogsgaard-Larsen P.

Abstract: The enantiomers of the glutamic acid central nervous system receptor agonist alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) were prepared via kinetic resolution of the racemic N-acetylated 3-methoxy derivative by reusable, immobilized aminoacylase. L-AMPA was more effective (IC50 = 0.6 microM) than D-AMPA (IC50 = 4.8 microM) in displacing racemic [3H]AMPA from binding sites on rat brain synaptic membranes in agreement with their relative in vivo excitatory potencies.

CiteXplore: 6133955

DOI: 10.1021/jm00360a021