Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors

J Pharmacol Exp Ther. 1994 Nov;271(2):735-40.

Abstract

Four pharmacological subtypes of the alpha-2 adrenergic receptor have been identified; however, only three subtypes exist in any given species. Although the alpha-2A adrenergic receptor, as defined by the human platelet, and the alpha-2D receptor, as defined in the bovine pineal, have very different pharmacological characteristics, they are more similar to each other than either is to the alpha-2B or alpha-2C subtype. The human alpha-2-C10 clone (alpha-2A) and the rat RG20 clone have an 89% identity in their predicted amino acid sequence and are considered to be species orthologs. Although the expressed RG20 clone appears to have alpha-2D pharmacology, a careful comparison of its pharmacological characteristics with the bovine pineal has not been reported previously. Based on the pKi values of a panel of 13 alpha-2 adrenergic agents that have been used previously to compare the alpha-2A, alpha-2B and alpha-2C subtypes, the pharmacological characteristics of the bovine pineal alpha-2D receptor appear to be very similar to the rat RG20 clone (correlation coefficient, r, of 0.93). The porcine ortholog of the human alpha-2-C10 receptor has pharmacological characteristics identical to the human alpha-2A receptor (r = 0.99). Because of its higher affinity for the alpha-2D receptor, [3H]RX821002 is a better radioligand than [3H]rauwolscine for studying this receptor subtype.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Binding Sites
  • Cattle
  • Cell Line
  • Dioxanes / metabolism
  • Humans
  • Idazoxan / analogs & derivatives
  • Rats
  • Receptors, Adrenergic, alpha-2 / chemistry
  • Receptors, Adrenergic, alpha-2 / classification*
  • Receptors, Adrenergic, alpha-2 / metabolism
  • Species Specificity
  • Swine
  • Yohimbine / metabolism

Substances

  • Dioxanes
  • Receptors, Adrenergic, alpha-2
  • Yohimbine
  • 2-methoxyidazoxan
  • Idazoxan