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, John W Regan, R. J. Lefkowitz, M. G. Caron

Research output: Contribution to journalArticle

18 Citations (Scopus)

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 α2-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-(allyl-oxy)-6-chloro-3-methyl-2,3,4,5-tetrahydro-l//-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-1H-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
StatePublished - 1984
Externally publishedYes

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Platelets
Adrenergic Receptors
Purification
Blood Platelets
Ligands
Membranes
Benzazepines
Enzymes
Adenylyl Cyclases
Molecules
benalfocin

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

DeMarinis, R. M., Krog, A. J., Shah, D. H., Lafferty, J., Holden, K. G., Hieble, J. P., ... 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.

Development of an affinity ligand for purification of α2-adrenoceptors from human platelet membranes. / DeMarinis, R. M.; Krog, A. J.; Shah, D. H.; Lafferty, J.; Holden, K. G.; Hieble, J. P.; Matthews, W. D.; Regan, John W; Lefkowitz, R. J.; Caron, M. G.

In: Journal of Medicinal Chemistry, Vol. 27, No. 7, 1984, p. 918-921.

Research output: Contribution to journalArticle

DeMarinis, RM, Krog, AJ, Shah, DH, Lafferty, J, Holden, KG, Hieble, JP, Matthews, WD, Regan, JW, Lefkowitz, RJ & Caron, MG 1984, 'Development of an affinity ligand for purification of α2-adrenoceptors from human platelet membranes', Journal of Medicinal Chemistry, vol. 27, no. 7, pp. 918-921.
DeMarinis RM, Krog AJ, Shah DH, Lafferty J, Holden KG, Hieble JP et al. Development of an affinity ligand for purification of α2-adrenoceptors from human platelet membranes. Journal of Medicinal Chemistry. 1984;27(7):918-921.
DeMarinis, R. M. ; Krog, A. J. ; Shah, D. H. ; Lafferty, J. ; Holden, K. G. ; Hieble, J. P. ; Matthews, W. D. ; Regan, John W ; Lefkowitz, R. J. ; Caron, M. G. / Development of an affinity ligand for purification of α2-adrenoceptors from human platelet membranes. In: Journal of Medicinal Chemistry. 1984 ; Vol. 27, No. 7. pp. 918-921.
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AU - Krog, A. J.

AU - Shah, D. H.

AU - Lafferty, J.

AU - Holden, K. G.

AU - Hieble, J. P.

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AU - Regan, John W

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