skip to main content

Title: Angiotensin II receptor heterogeneity

The possibility of receptor heterogeneity in the angiotensin II (AII) system has been suggested previously, based on differences in Kd values or sensitivity to thiol reagents. One of the authors earliest indications was the frequent observation of incomplete inhibition of the binding of AII to adrenal cortical membranes. Autoradiographic studies demonstrated that all of the labeling of the rat adrenal was blocked by unlabeled AII or saralasin, but not by DuP 753. The predominant receptor in the rat adrenal cortex (80%) is sensitive to dithiothreitol (DTT) and DuP 753, and is designated AII-1. The residual sites in the adrenal cortex and almost all of the sites in the rat adrenal medulla are insensitive to both DTT and DuP 753, but were blocked by EXP655. These sites have been confirmed by ligand binding studies and are designated AII-2. The rabbit adrenal cortex is unique in yielding a nonuniform distribution of AII-2 sites around the outer layer of glomerulosa cells. In the rabbit kidney, the sites on the glomeruli are AII-1, but the sites on the kidney capsule are AII-2. Angiotensin III appears to have a higher affinity for AII-2 sites since it inhibits the binding to the rabbit kidney capsule butmore » not the glomeruli. Elucidation of the distribution and function of these diverse sites should permit the development of more selective and specific therapeutic strategies.« less
Authors:
; ; ; ; ; ; ; ; ;  [1]
  1. (DuPont Merck Pharmaceutical Company, Wilmington, DE (USA))
Publication Date:
OSTI Identifier:
5229566
Resource Type:
Journal Article
Resource Relation:
Journal Name: American Journal of Hypertension; (United States); Journal Volume: 4:4 Pt 2
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; ANGIOTENSIN; RECEPTORS; TISSUE DISTRIBUTION; ADRENAL GLANDS; AFFINITY; AUTORADIOGRAPHY; BIOCHEMICAL REACTION KINETICS; CELL MEMBRANES; IODINE ISOTOPES; KIDNEYS; MICROSOMES; RABBITS; RATS; ANIMALS; BODY; CARDIOVASCULAR AGENTS; CELL CONSTITUENTS; DISTRIBUTION; DRUGS; ENDOCRINE GLANDS; GLANDS; GLOBULINS; ISOTOPES; KINETICS; MAMMALS; MEMBRANE PROTEINS; MEMBRANES; ORGANIC COMPOUNDS; ORGANS; PROTEINS; REACTION KINETICS; RIBOSOMES; RODENTS; VASOCONSTRICTORS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques