Development of an Affinity Ligand for Purification of α2-Adrenoceptors from Human Platelet Membranes

R. M. DeMarinis, A. J. Krog, D. H. Shah, J. Lafferty, K. G. Holden, J. P. Hieble, W. D. Matthews, J. W. Regan, R. J. Lefkowitz, M. G. Caron

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Abstract

Human platelets contain α2-adrenoceptors which are negatively coupled to the enzyme adenylate cyclase. In order to better understand the interaction of this subtype of α receptor with this key enzyme, we have initiated a program to isolate and characterize the a2-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 α2-adrenoceptor antagonist, which was obtained by synthetic modification of 6-chloro-3-methyl-2, 3,4, 5-tetrahydro-lH-3-benzazepine (SK&F 86466), a novel antagonist with high affinity for the α2-receptor.

Original languageEnglish (US)
Pages (from-to)918-921
Number of pages4
JournalJournal of Medicinal Chemistry
Volume27
Issue number7
DOIs
StatePublished - Oct 1984
Externally publishedYes

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

DeMarinis, R. M., Krog, A. J., Shah, D. H., Lafferty, J., Holden, K. G., Hieble, J. P., Matthews, W. D., Regan, J. W., Lefkowitz, R. J., & Caron, M. G. (1984). Development of an Affinity Ligand for Purification of α2-Adrenoceptors from Human Platelet Membranes. Journal of Medicinal Chemistry, 27(7), 918-921. https://doi.org/10.1021/jm00373a018