title: 1S,3R-ACPD-sensitive (metabotropic) [3H]glutamate receptor binding in membranes.
abstract: Metabotropic glutamate receptors are selectively activated by 1S,3R-1-aminocyclopentane-1,3-dicarboxylic acid (1S,3R-ACPD). [3H]Glutamate binding sites in rat brain membranes were characterized in the presence of (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), kainate, and N-methyl-D-aspartate (NMDA) to block binding to ionotropic glutamate receptors. 1S,3R-ACPD displaced a single population of [3H]glutamate binding sites and was mimicked by other metabotropic glutamate agonists with a potency order of L-glutamate > 1S,3R-ACPD > ibotenate > 1R,3S-ACPD. Quisqualate interacted at two populations of binding sites. 1S,3R-ACPD-sensitive [3H]glutamate binding was saturable (Bmax = 2.50 +/- 0.27 pmol/mg protein), reversible, and had high-affinity (KD = 187 +/- 60 nM). 1S,3R-ACPD-sensitive [3H]glutamate binding likely represents labeling of metabotropic glutamate receptors in rat brain membranes.
authors.affiliation: CNS Research, Eli Lilly and Company, Indianapolis, IN 46285.
authors.forename: D D
authors.initials: DD
authors.lastname: Schoepp
authors.forename: R A
authors.initials: RA
authors.lastname: True
mesh_terms: D000818:Animals; D002540:Cerebral Cortex / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D003515:Cycloleucine / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D017470:Receptors, Glutamate / Q000187:drug effects*
chemical_list: D017470:Receptors, Glutamate; D003515:Cycloleucine; C036361:1-amino-1,3-dicarboxycyclopentane