Arylazide photoaffinity probe for α2-adrenoceptors

John W. Regan, Robert M. DeMarinis, Robert J. Lefkowitz

Research output: Contribution to journalArticle

5 Scopus citations

Abstract

An arylazide photoaffinity probe for α2-adrenoceptors has been developed and characterized. The compound, 3-methyl-6-chloro-9-azido-1H-2,3,4,5-tetrahydro-3-benzazepine (SKF 102229), had a Ki for the human platelet α2-adrenoceptor of ~40 nM. Upon exposure to ultraviolet light, SKF 102229 irreversibly blocked the binding of [3H]yohimbine to both membrane bound and solubilized, partially purified, receptors. The extent of α2-adrenoceptor blockade was dependent upon both the length of exposure to ultraviolet light and the concentration of SKF 102229. Typically, a 60% decrease in α2-adrenoceptor number is obtained following 8 min of photolysis in the presence of 100 nM SKF 102229. The pharmacologic characteristics of the irreversible blockade produced by SKF 102229 were those of an α2-adrenoceptor. Thus, photodependent, irreversible blockade of α2-adrenoceptors by SKF 102229 was prevented by the concomitant presence of phentolamine or p-aminoclonidine but not by prazosin. Given its specificity and efficient blockade of the ligand binding site, SKF 102229 should prove useful for studies of the structure and function of α2-adrenoceptors.

Original languageEnglish (US)
Pages (from-to)3667-3672
Number of pages6
JournalBiochemical Pharmacology
Volume34
Issue number20
DOIs
StatePublished - Oct 15 1985
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology

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