The selectivity of newly synthesized ergot derivatives to alpha 1- and alpha 2-adrenoceptors, D1- and D2-dopaminergic receptors, muscarinic acetylcholinoceptors and beta-adrenoceptors

Gen Pharmacol. 1988;19(3):463-6. doi: 10.1016/0306-3623(88)90048-1.

Abstract

1. We tested affinities of newly synthesized ergot derivatives to alpha 1- and alpha 2-adrenoceptors, D1- and D2-dopamine receptors, muscarinic acetylcholinoceptors and beta-adrenoceptors using radioligand binding techniques. 2. BAM-1110 was alpha 2-selective, though its affinity to alpha 2-adrenoceptors was one tenth less than that of yohimbine. 3. BAM-1303, which was non-selective, had high affinity to alpha-adrenoceptors. The pKi-values for BAM-1303 was 10.11 against both [3H]prazosin (alpha 1-ligand) and [3H]rauwolscine (alpha 2-ligand). 4. New ergot derivatives were selective to D2-dopamine receptors. BAM-1125 and BAM-1303 had high selectivity to D2-receptors. 5. They had less affinity to muscarinic receptors and beta-adrenoceptors.

MeSH terms

  • Animals
  • Binding, Competitive
  • Cerebral Cortex / metabolism
  • Ergot Alkaloids / metabolism*
  • In Vitro Techniques
  • Male
  • Radioligand Assay
  • Rats
  • Rats, Inbred Strains
  • Receptors, Adrenergic, alpha / metabolism*
  • Receptors, Adrenergic, beta / metabolism*
  • Receptors, Dopamine / metabolism*
  • Receptors, Muscarinic / metabolism*

Substances

  • Ergot Alkaloids
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic, beta
  • Receptors, Dopamine
  • Receptors, Muscarinic