Identification of drugs subtype-selective for alpha 2A-, alpha 2B-, and alpha 2C-adrenoceptors in the pig cerebellum and kidney cortex

Eur J Pharmacol. 1995 Sep 25;284(3):271-9. doi: 10.1016/0014-2999(95)00354-n.

Abstract

The radioligands [3H]MK912 and [3H]RX821002 were used to label alpha2A-, alpha2B-, and alpha2C-adrenoceptors of the pig cerebellum and kidney cortex. By inclusion of the alpha2A-adrenoceptor-selective drug, BRL44408, and using a 'multi-curve' experimental design all the three porcine alpha2-adrenoceptor subtypes could be characterized pharmacologically. The data indicate that the pig alpha2-adrenoceptor subtypes are pharmacologically more related to human alpha2-adrenoceptor subtypes than to the rodent alpha2-adrenoceptors. We suggest a set of drugs that are useful for the delineation of the pig alpha2-adrenoceptor subtypes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive
  • Cerebellum / chemistry*
  • Dibenzazepines / metabolism
  • Dioxanes / metabolism
  • Idazoxan / analogs & derivatives
  • Imidazoles / metabolism
  • Kidney Cortex / chemistry*
  • Quinolizines / metabolism
  • Receptors, Adrenergic, alpha-2 / classification*
  • Receptors, Adrenergic, alpha-2 / metabolism
  • Swine

Substances

  • Dibenzazepines
  • Dioxanes
  • Imidazoles
  • Quinolizines
  • Receptors, Adrenergic, alpha-2
  • L 657743
  • BRL 41992
  • 2-methoxyidazoxan
  • Idazoxan