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1‐Aminocyclopropane Carboxylic Acid: A Potent and Selective Ligand for the Glycine Modulatory Site of the N‐Methyl‐ d ‐Aspartate Receptor Complex
Author(s) -
Marvizón JuanCarlos G.,
Lewin Anita H.,
Skolnick Phil
Publication year - 1989
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1989.tb02554.x
Subject(s) - glycine , chemistry , glycine receptor , 1 aminocyclopropane 1 carboxylic acid , ligand (biochemistry) , receptor , stereochemistry , biochemistry , amino acid , enzyme , biosynthesis
1‐Aminocyclopropane carboxylic acid (ACPC) competitively inhibited (IC 50 , 38 ± 7 n M ) [ 3 H]glycine binding to rat forebrain membranes but did not affect [ 3 H]strychnine binding to rat brainstem/ spinal cord membranes. Like glycine, ACPC enhanced 3 H‐labelled (+)‐5‐methyl‐10,11 ‐dihydro‐5 H ‐dibenzo[ a, d ]cyclohepten‐5,10‐imine maleate ([ 3 H]MK‐801) binding to TV‐methyl‐D‐aspartate receptor‐coupled cation channels (EC 50 , 135 ± 76 n M and 206 ± 78 n M for ACPC and glycine, respectively) but was ∼ 40% less efficacious in this regard. The maximum increase in [ 3 H]MK‐801 binding produced by a combination of ACPC and glycine was not different from that elicited by glycine, but both compounds potentiated glutamate‐stimulated [ 3 H]MK‐801 binding. These findings indicate that ACPC is a potent and selective ligand at the glycine modulatory site associated with the N ‐methyl‐ d ‐aspartate receptor complex.