Article date: 1991/8/14
PubMed ID: 1664338
Journal name: European journal of pharmacology (ISSN: 0014-2999)
(1S,3R)-1-Aminocyclopentane-1,3-dicarboxylic acid (1S,3R-ACPD) and (1R,3S)-1-aminocyclopentane-1,3-dicarboxylic acid (1R,3S-ACPD) were characterized for potency, efficacy, and selectivity at metabotropic excitatory amino acid receptors. 1S,3R-ACPD stimulated [3H]phosphoinositide hydrolysis in slices of the neonatal and adult rat hippocampus with full efficacy and twice the potency relative to what has been shown for (+/-)-trans-ACPD. 1S,3R-ACPD was up to 30 times more potent in activating metabotropic excitatory amino acid receptors, compared to its affinity for [3H]CGS19755 binding to NMDA receptors. In contrast, 1R,3S-ACPD was much less potent, efficacious, and selective than 1S,3R-ACPD. Although 1S,3R-ACPD is not specific, it is a most selective and efficacious agonist at metabotropic excitatory amino acid receptors.
Author List: Schoepp D D, Johnson B G, True R A, Monn J A
Publication Types: Comparative Study; Journal Article
Substances mentioned in the article: Phosphatidylinositols; Receptors, Amino Acid; Receptors, Cell Surface; Cycloleucine; 1-amino-1,3-dicarboxycyclopentane; Ibotenic Acid; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid; Kainic Acid;
Mesh terms: Animals; Brain/drug effects; Cycloleucine/analogs & derivatives; Hydrolysis/drug effects; Ibotenic Acid/analogs & derivatives; Kainic Acid/metabolism; Male; Membranes/metabolism; Phosphatidylinositols/metabolism; Rats; Rats, Inbred Strains; Receptors, Amino Acid; Receptors, Cell Surface/metabolism; Stimulation, Chemical; alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid;