[125I][D-Tyr25,Nle28,31]CCK-(25-33): a convenient new aminopeptidase resistant cholecystokinin analogue for radioligand binding and autoradiography.
The 125I-labeled sulfated cholecystokinin (CCK) analogue, [D-Tyr25,Nle28,31]CCK-(25-33), bound saturably to membranes from rat cerebral cortex and to brain tissue sections. Competition studies suggested binding to sites of the CCKB subtypes. The high affinity for brain membranes (Kd = 0.14 nM) and high specific binding to brain sections (80-90% specific binding), as well as its high specific radioactivity, makes it a suitable ligand for autoradiographic studies of cholecystokinin receptors.
Carlberg
M
M
University of Melbourne, Clinical Pharmacology and Therapeutics Unit, Austin Hospital, Heidelberg, Victoria, Australia.
Beart
P M
PM
Jarrott
B
B
D000626:Aminopeptidases / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000378:metabolism; D002766:Cholecystokinin / Q000031:analogs & derivatives* / Q000378:metabolism; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D010446:Peptide Fragments / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011949:Receptors, Cholecystokinin / Q000378:metabolism
D010446:Peptide Fragments; D011949:Receptors, Cholecystokinin; C068406:cholecystokinin (25-33), Tyr(25)-Nle(28,31)-; D002766:Cholecystokinin; D000626:Aminopeptidases