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

Publication ,  Journal Article
DeMarinis, RM; Krog, AJ; Shah, DH; Lafferty, J; Holden, KG; Hieble, JP; Matthews, WD; Regan, JW; Lefkowitz, RJ; Caron, MG
Published in: J Med Chem
July 1984

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.

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Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

July 1984

Volume

27

Issue

7

Start / End Page

918 / 921

Location

United States

Related Subject Headings

  • Yohimbine
  • Synaptic Transmission
  • Structure-Activity Relationship
  • Receptors, Adrenergic, alpha
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Guinea Pigs
  • Cell Membrane
  • Blood Platelets
  • Benzazepines
 

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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 alpha 2-adrenoceptors from human platelet membranes. J Med Chem, 27(7), 918–921. https://doi.org/10.1021/jm00373a018
DeMarinis, R. M., A. J. Krog, D. H. Shah, J. Lafferty, K. G. Holden, J. P. Hieble, W. D. Matthews, J. W. Regan, R. J. Lefkowitz, and M. G. Caron. “Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.J Med Chem 27, no. 7 (July 1984): 918–21. https://doi.org/10.1021/jm00373a018.
DeMarinis RM, Krog AJ, Shah DH, Lafferty J, Holden KG, Hieble JP, et al. Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes. J Med Chem. 1984 Jul;27(7):918–21.
DeMarinis, R. M., et al. “Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes.J Med Chem, vol. 27, no. 7, July 1984, pp. 918–21. Pubmed, doi:10.1021/jm00373a018.
DeMarinis RM, Krog AJ, Shah DH, Lafferty J, Holden KG, Hieble JP, Matthews WD, Regan JW, Lefkowitz RJ, Caron MG. Development of an affinity ligand for purification of alpha 2-adrenoceptors from human platelet membranes. J Med Chem. 1984 Jul;27(7):918–921.
Journal cover image

Published In

J Med Chem

DOI

ISSN

0022-2623

Publication Date

July 1984

Volume

27

Issue

7

Start / End Page

918 / 921

Location

United States

Related Subject Headings

  • Yohimbine
  • Synaptic Transmission
  • Structure-Activity Relationship
  • Receptors, Adrenergic, alpha
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Guinea Pigs
  • Cell Membrane
  • Blood Platelets
  • Benzazepines