Identification of angiotensin II receptor subtypes

Journal Article · Thu Nov 30 04:00:00 EST 1989 · Biochemical and Biophysical Research Communications; (USA)

DOI:https://doi.org/10.1016/0006-291X(89)91054-1· OSTI ID:5031475

Chiu, A T; Herblin, W F; McCall, D E; Ardecky, R J; Carini, D J; Duncia, J V; Pease, L J; Wong, P C; Wexler, R R; Johnson, A L

We have demonstrated the existence of two distinct subtypes of the angiotensin II receptor in the rat adrenal gland using radioligand binding and tissue section autoradiography. The identification of the subtypes was made possible by the discovery of two structurally dissimilar, nonpeptide compounds, DuP 753 and EXP655, that show reciprocal selectivity for the two subtypes. In the rat adrenal cortex, DuP 753 inhibited 80% of the total AII binding with an IC50 value on the sensitive sites of 2 x 10(-8) M, while EXP655 displaced only 20%. In the rat adrenal medulla, EXP655 gave 90% inhibition of AII binding with an IC50 value of 3.0 x 10(-8) M, while DuP 753 was essentially inactive. The combination of the two compounds completely inhibited AII binding in both tissues.

• OSTI ID: 5031475
• Journal Information: Biochemical and Biophysical Research Communications; (USA), Journal Name: Biochemical and Biophysical Research Communications; (USA) Vol. 165:1; ISSN BBRCA; ISSN 0006-291X
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ADRENAL GLANDS
ANGIOTENSIN
ANIMALS
AUTORADIOGRAPHY
BIOCHEMICAL REACTION KINETICS
BODY
CARDIOVASCULAR AGENTS
CELL CONSTITUENTS
DRUGS
ENDOCRINE GLANDS
GLANDS
GLOBULINS
IODINE ISOTOPES
ISOTOPES
KINETICS
MAMMALS
MEMBRANE PROTEINS
MICROSOMES
MOLECULAR STRUCTURE
ORGANIC COMPOUNDS
ORGANOIDS
ORGANS
PROTEINS
RATS
REACTION KINETICS
RECEPTORS
RIBOSOMES
RODENTS
VASOCONSTRICTORS
VERTEBRATES