Chronic proglumide increases [3H]spiperone binding in the rat brain.
The cholecystokinin (CCK) antagonist, proglumide, administered chronically (41.0-53.5 mg/kg per day, 14 days) to rats via osmotic mini-pumps, produced a significant 13% increase in the number of [3H]spiperone labeled binding sites (Bmax) in the striatum. There was no associated change in the affinity (Kd) of [3H]spiperone for the striatal binding sites. Given chronically at lower dose levels (10.4-13.6 or 21.8-29.8 mg/kg per day), or acutely in doses of 10, 20 or 40 mg/kg s.c., proglumide failed to alter the binding of [3H]spiperone to rat striatal tissue. These data indicate long-term proglumide administration increases the number of binding sites for [3H]spiperone, thought to be a ligand for dopamine D-2 receptors.
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D002090:Butyrophenones / Q000378:metabolism*; D002766:Cholecystokinin / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism; D005973:Glutamine / Q000031:analogs & derivatives*; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D011377:Proglumide / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000378:metabolism; D013134:Spiperone / Q000378:metabolism*
D002090:Butyrophenones; D011954:Receptors, Dopamine; D005973:Glutamine; D013134:Spiperone; D002766:Cholecystokinin; D011377:Proglumide