( sup 3 H)DUP 753, a highly potent and specific radioligand for the angiotensin II-1 receptor subtype
- E.I. du Pont de Nemours Company, Wilmington, DE (USA)
({sup 3}H)Dup 753, a nonpeptide angiotensin II (AII) receptor antagonist radioligand, was used to characterize a subtype of AII receptors in rat adrenal cortical microsomes. By Scatchard analysis, a single class of DuP 753 binding sites was found with an affinity of 6.4 nM and a Bmax of 1.3 pmol/mg protein. These sites were saturable and readily reversible. Angiotensin (I, II, III) expressed the same affinities and order of potency for these binding sites as those labeled by ({sup 3}H)AII for the AII-1 sites. The affinities expressed by nonpeptide AII antagonists were commensurate with their inhibitory potencies on AII-1 receptors. PD123177, an AII-2 specific ligand, and other non-AII peptides showed no inhibitory action. These data together with the differential tissue distribution strongly support our conclusion that ({sup 3}H)DuP 753 is a potent and highly specific radioligand for the AII-1 receptors.
- OSTI ID:
- 6276024
- Journal Information:
- Biochemical and Biophysical Research Communications; (USA), Vol. 172:3; ISSN 0006-291X
- Country of Publication:
- United States
- Language:
- English
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550201* - Biochemistry- Tracer Techniques