Covalent labeling of the cerebral cortex alpha 1-adrenergic receptor with a new high affinity radioiodinated photoaffinity probe.

Journal Article (Journal Article)

A novel high affinity radioiodinated photoaffinity probe, 4-amino-6,7-dimethoxy-2[4-[5(3-[125I]iodo-4-azidophenyl)pentanoyl]-1- piperazinyl]-quinazoline, structurally related to the potent alpha 1-adrenergic antagonist prazosin, was developed and used to covalently label the rat cerebral cortex alpha 1-adrenergic receptor. In the absence of light, this ligand binds to cortex plasma membranes with a dissociation constant of 308 pM and with a maximal number of binding sites of 200 fmol/mg protein. Upon photolysis, the ligand incorporates irreversibly into plasma membrane proteins. Autoradiograms of such membrane samples subjected to sodium dodecyl sulfate-polyacrylamide gel electrophoresis reveal a major specifically labeled polypeptide at Mr = 79,000. The covalent incorporation into the peptide at Mr = 79,000 can be inhibited by several adrenergic receptor ligands with a typical alpha 1-adrenergic receptor specificity and stereoselectivity.

Full Text

Duke Authors

Cited Authors

  • Leeb-Lundberg, LM; Dickinson, KE; Heald, SL; Wikberg, JE; DeBernardis, JF; Winn, M; Arendsen, DL; Lefkowitz, RJ; Caron, MG

Published Date

  • September 30, 1983

Published In

Volume / Issue

  • 115 / 3

Start / End Page

  • 946 - 951

PubMed ID

  • 6313003

International Standard Serial Number (ISSN)

  • 0006-291X

Digital Object Identifier (DOI)

  • 10.1016/s0006-291x(83)80026-6


  • eng

Conference Location

  • United States