Specific binding of D-Tyr25 (Nle28,31)-CCK(25-33) to cortical membranes from rat brain.
The 125I-labeled sulfonated cholecystokinin (CCK) analogue, D-Tyr25(Nle28,31)-CCK(25-33), bound saturably and reversibly to membranes of rat cerebral cortex. The dissociation constant Kd was estimated to be 0.14 nM by Scatchard analysis and 0.40 nM from analyses of dissociation/association rates. Hill coefficients of 0.99, Scatchard plots and drug competition studies were consistent with a single population of binding sites. Dependence on divalent cations and inhibition by guanylyl-imidodiphosphate suggested binding to a receptor coupled to a G protein. Competition studies with CCK-analogues and non-peptide specific antagonists indicated binding to receptor sites of the B-subtype (CCKB).
Carlberg
M
M
University of Melbourne, Clinical Pharmacology and Therapeutics Unit, Austin Hospital, Heidelberg, Vic.
Jarrott
B
B
Beart
P M
PM
D000818:Animals; D001570:Benzodiazepinones / Q000378:metabolism; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism*; D002766:Cholecystokinin / Q000031:analogs & derivatives* / Q000378:metabolism; D006207:Half-Life; D066298:In Vitro Techniques; D007457:Iodine Radioisotopes; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D010446:Peptide Fragments / Q000378:metabolism*; D010671:Phenylurea Compounds; D051381:Rats; D011919:Rats, Inbred Strains; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors / Q000378:metabolism
D001570:Benzodiazepinones; D007457:Iodine Radioisotopes; D010446:Peptide Fragments; D010671:Phenylurea Compounds; D011949:Receptors, Cholecystokinin; C068406:cholecystokinin (25-33), Tyr(25)-Nle(28,31)-; C058121:L 365260; D002766:Cholecystokinin