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Molecular Pharmacology, Vol 18, 210-214, Copyright © 1980 by the American Society for Pharmacology and Experimental Therapeutics

Affinity Labeling of Angiotensin II Receptors in the Isolated Rat Uterus with a Photolabile Antagonist

Y. C. KWOK 1 and G. J. MOORE 1

1 Department of Pharmacology and Therapeutics, The University of Calgary, Calgary, Canada T2N 1N4

[4-Azidobenzoic acid1, isoleucine8]angiotensin II was synthesized by the solid phase method and purified by carboxymethyl cellulose chromatography. In the dark, this peptide acted as a potent competitive antagonist of angiotensin II on the isolated rat uterus (pA2 = 8.1). Irradiation of the tissue with ultraviolet light in the presence of the analog resulted in irreversible blockade of the response to angiotensin II but not to oxytocin. The photoaffinity labeling procedure resulted in a shift of the dose-response curve for angiotensin II without a loss of the maximum response, suggesting the existence of spare receptors for angiotensin II in uterine smooth muscle.

Submitted on December 5, 1979
Accepted on March 13, 1980






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