( sup 3 H)DUP 753, a highly potent and specific radioligand for the angiotensin II-1 receptor subtype

Journal Article · Thu Nov 15 04:00:00 EST 1990 · Biochemical and Biophysical Research Communications; (USA)

DOI:https://doi.org/10.1016/0006-291X(90)91575-D· OSTI ID:6276024

Chiu, A T; McCall, D E; Aldrich, P E; Timmermans, P B ^[1]

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1. 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), Journal Name: Biochemical and Biophysical Research Communications; (USA) Vol. 172:3; ISSN BBRCA; ISSN 0006-291X
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ADRENAL GLANDS
AFFINITY
ANGIOTENSIN
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CARDIOVASCULAR AGENTS
CELL CONSTITUENTS
CHEMICAL COMPOSITION
DISTRIBUTION
DRUGS
ENDOCRINE GLANDS
GLANDS
GLOBULINS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LIGANDS
MAMMALS
MEMBRANE PROTEINS
MICROSOMES
ORGANIC COMPOUNDS
ORGANOIDS
ORGANS
PROTEINS
RATS
REACTION KINETICS
RECEPTORS
RIBOSOMES
RODENTS
TISSUE DISTRIBUTION
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VASOCONSTRICTORS
VERTEBRATES