Arylazide photoaffinity probe for alpha 2-adrenoceptors.

Published

Journal Article

An arylazide photoaffinity probe for alpha 2-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 alpha 2-adrenoceptor of approximately 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 alpha 2-adrenoceptor blockade was dependent upon both the length of exposure to ultraviolet light and the concentration of SKF 102229. Typically, a 60% decrease in alpha 2-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 alpha 2-adrenoceptor. Thus, photodependent, irreversible blockade of alpha 2-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 alpha 2-adrenoceptors.

Full Text

Duke Authors

Cited Authors

  • Regan, JW; DeMarinis, RM; Lefkowitz, RJ

Published Date

  • October 1, 1985

Published In

Volume / Issue

  • 34 / 20

Start / End Page

  • 3667 - 3672

PubMed ID

  • 2864929

Pubmed Central ID

  • 2864929

Electronic International Standard Serial Number (EISSN)

  • 1873-2968

International Standard Serial Number (ISSN)

  • 0006-2952

Digital Object Identifier (DOI)

  • 10.1016/0006-2952(85)90228-x

Language

  • eng