The selectivity of some ergot derivatives for alpha 1 and alpha 2-adrenoceptors of rat cerebral cortex

Eur J Pharmacol. 1983 Aug 5;91(4):363-9. doi: 10.1016/0014-2999(83)90159-0.

Abstract

The affinities of several ergot derivatives for rat cerebral cortex alpha 1- and alpha 2-adrenoceptors were assessed using radioligand binding techniques. In most cases both [3H]prazosin (labelling alpha 1-adrenoceptors) and [3H]rauwolscine (labelling alpha 2-adrenoceptors) binding were displaced by the ergot derivatives tested, but with markedly different potency. Generally compounds displayed selectivity toward the alpha 2-adrenoceptor, particularly CQ 32-084, which had a Ki value against [3H]rauwolscine binding of 35 nM, but had little effect on [3H]prazosin binding at concentrations in excess of 5 microM. Lisuride was the most potent displacer of [3H]rauwolscine binding with a Ki value of 0.54 nM. Only bromocriptine was relatively alpha 1-selective with a Ki against [3H]prazosin binding of 18 nM and against [3H]rauwolscine binding of 120 nM. The results indicate that the ergot derivatives tested display a marked affinity for alpha-adrenoceptors and that their actions at this receptor class should be considered when interpreting their pharmacological activity in vivo.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cerebral Cortex / drug effects*
  • Ergolines / pharmacology
  • Ergot Alkaloids / pharmacology*
  • Female
  • In Vitro Techniques
  • Kinetics
  • Lisuride / pharmacology
  • Male
  • Membranes / metabolism
  • Prazosin / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, alpha / classification
  • Receptors, Adrenergic, alpha / drug effects*
  • Yohimbine / metabolism

Substances

  • Ergolines
  • Ergot Alkaloids
  • Receptors, Adrenergic, alpha
  • etisulergine
  • Yohimbine
  • Lisuride
  • Prazosin