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Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.

Publication ,  Journal Article
Bylund, DB; Blaxall, HS; Iversen, LJ; Caron, MG; Lefkowitz, RJ; Lomasney, JW
Published in: Mol Pharmacol
July 1992

On the basis of extensive radioligand data and more limited functional data, three pharmacological subtypes of alpha 2-adrenergic receptors have been identified. More recently, three human genes or cDNAs for alpha 2-adrenergic receptors have been identified by molecular cloning. The relationship, however, among the pharmacologically defined subtypes and those identified by molecular cloning has not been clear. In order to resolve this issue, we have compared the pharmacological characteristics of the receptors identified by molecular cloning and expressed in COS-7 cells with the characteristics of the pharmacologically defined receptors in their respective prototypic tissue or cell line. The affinities (Ki values) of 12 subtype-selective alpha 2-adrenergic antagonists were determined for the alpha 2 receptor in the six preparations, by radioligand binding. Correlation analyses of the pKi values indicate that the alpha 2A subtype, as defined in the HT29 cell line, the alpha 2B receptor of the neonatal rat lung, and the alpha 2C subtype, as defined in an oppossum kidney cell line, correspond to the cloned human alpha 2-C10, alpha 2-C2, and alpha 2-C4 receptor subtypes, respectively.

Duke Scholars

Published In

Mol Pharmacol

ISSN

0026-895X

Publication Date

July 1992

Volume

42

Issue

1

Start / End Page

1 / 5

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Receptors, Adrenergic, alpha
  • Rats, Inbred Strains
  • Rats
  • Radioligand Assay
  • Pharmacology & Pharmacy
  • Lung
  • Humans
  • DNA
  • Cloning, Molecular
 

Citation

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MLA
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Bylund, D. B., Blaxall, H. S., Iversen, L. J., Caron, M. G., Lefkowitz, R. J., & Lomasney, J. W. (1992). Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol, 42(1), 1–5.
Bylund, D. B., H. S. Blaxall, L. J. Iversen, M. G. Caron, R. J. Lefkowitz, and J. W. Lomasney. “Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning.Mol Pharmacol 42, no. 1 (July 1992): 1–5.
Bylund DB, Blaxall HS, Iversen LJ, Caron MG, Lefkowitz RJ, Lomasney JW. Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol. 1992 Jul;42(1):1–5.
Bylund DB, Blaxall HS, Iversen LJ, Caron MG, Lefkowitz RJ, Lomasney JW. Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol. 1992 Jul;42(1):1–5.

Published In

Mol Pharmacol

ISSN

0026-895X

Publication Date

July 1992

Volume

42

Issue

1

Start / End Page

1 / 5

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Receptors, Adrenergic, alpha
  • Rats, Inbred Strains
  • Rats
  • Radioligand Assay
  • Pharmacology & Pharmacy
  • Lung
  • Humans
  • DNA
  • Cloning, Molecular