Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.


Journal Article

Human platelets contain alpha 2-adrenoceptors which are negatively coupled to the enzyme adenylate cyclase. In order to better understand the interaction of this subtype of alpha receptor with this key enzyme, we have initiated a program to isolate and characterize the alpha 2-adrenoceptor. This report describes the synthesis and biological characterization of a series of molecules that were prepared as affinity ligands for this purpose. The best of these is 9-(allyloxy)-6-chloro-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SK&F 101253). This compound is an alpha 2-adrenoceptor antagonist, which was obtained by synthetic modification of 6-chloro-3-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SK&F 86466), a novel antagonist with high affinity for the alpha 2-receptor.

Full Text

Duke Authors

Cited Authors

  • DeMarinis, RM; Krog, AJ; Shah, DH; Lafferty, J; Holden, KG; Hieble, JP; Matthews, WD; Regan, JW; Lefkowitz, RJ; Caron, MG

Published Date

  • July 1, 1984

Published In

Volume / Issue

  • 27 / 7

Start / End Page

  • 918 - 921

PubMed ID

  • 6330361

Pubmed Central ID

  • 6330361

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm00373a018


  • eng

Conference Location

  • United States