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Arylazide photoaffinity probe for alpha 2-adrenoceptors.

Publication ,  Journal Article
Regan, JW; DeMarinis, RM; Lefkowitz, RJ
Published in: Biochem Pharmacol
October 15, 1985

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.

Duke Scholars

Published In

Biochem Pharmacol

DOI

ISSN

0006-2952

Publication Date

October 15, 1985

Volume

34

Issue

20

Start / End Page

3667 / 3672

Location

England

Related Subject Headings

  • Yohimbine
  • Ultraviolet Rays
  • Tritium
  • Receptors, Adrenergic, alpha
  • Prazosin
  • Photolysis
  • Phentolamine
  • Pharmacology & Pharmacy
  • Membranes
  • Humans
 

Citation

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Regan, J. W., DeMarinis, R. M., & Lefkowitz, R. J. (1985). Arylazide photoaffinity probe for alpha 2-adrenoceptors. Biochem Pharmacol, 34(20), 3667–3672. https://doi.org/10.1016/0006-2952(85)90228-x
Regan, J. W., R. M. DeMarinis, and R. J. Lefkowitz. “Arylazide photoaffinity probe for alpha 2-adrenoceptors.Biochem Pharmacol 34, no. 20 (October 15, 1985): 3667–72. https://doi.org/10.1016/0006-2952(85)90228-x.
Regan JW, DeMarinis RM, Lefkowitz RJ. Arylazide photoaffinity probe for alpha 2-adrenoceptors. Biochem Pharmacol. 1985 Oct 15;34(20):3667–72.
Regan, J. W., et al. “Arylazide photoaffinity probe for alpha 2-adrenoceptors.Biochem Pharmacol, vol. 34, no. 20, Oct. 1985, pp. 3667–72. Pubmed, doi:10.1016/0006-2952(85)90228-x.
Regan JW, DeMarinis RM, Lefkowitz RJ. Arylazide photoaffinity probe for alpha 2-adrenoceptors. Biochem Pharmacol. 1985 Oct 15;34(20):3667–3672.
Journal cover image

Published In

Biochem Pharmacol

DOI

ISSN

0006-2952

Publication Date

October 15, 1985

Volume

34

Issue

20

Start / End Page

3667 / 3672

Location

England

Related Subject Headings

  • Yohimbine
  • Ultraviolet Rays
  • Tritium
  • Receptors, Adrenergic, alpha
  • Prazosin
  • Photolysis
  • Phentolamine
  • Pharmacology & Pharmacy
  • Membranes
  • Humans