Receptor affinities of aporphine enantiomers in rat brain tissue

Eur J Pharmacol. 1994 Mar 11;254(1-2):199-203. doi: 10.1016/0014-2999(94)90388-3.

Abstract

R(-) and S(+) enantiomers of apomorphine, N-n-propylnorapomorphine and 11-hydroxy-N-n-propylnorapomorphine were screened for affinity at over 40 representative sites in rat brain tissue that included amine, purine, amino acid and peptide receptors, transporters, ion channels, and effector components; only dopamine receptors and alpha-adrenoceptors showed appreciable affinity that was quantified further. The aporphines showed R(-) > S(+) isomeric selectivity as well as D2 > D1 selectivity at dopamine receptors. While R(-) isomers preferred alpha 2-adrenoceptors, S(+)-aporphines were alpha 1-selective, with similar affinity at alpha 1-adrenoceptors and dopamine D2 receptors. Interactions of S(+)-aporphines at alpha 1-adrenoceptors as well as dopamine D2 receptors may contribute to their unusual behavioral properties.

Publication types

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

MeSH terms

  • Animals
  • Apomorphine / analogs & derivatives
  • Apomorphine / pharmacokinetics
  • Aporphines / pharmacokinetics*
  • Brain / metabolism*
  • Dopamine Agents / pharmacokinetics
  • In Vitro Techniques
  • Male
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Cell Surface / metabolism*
  • Receptors, Neurotransmitter / metabolism
  • Stereoisomerism

Substances

  • Aporphines
  • Dopamine Agents
  • Receptors, Cell Surface
  • Receptors, Neurotransmitter
  • N-n-propylnorapomorphine
  • 11-hydroxy-N-(n-propyl)noraporphine
  • Apomorphine