Selective binding of YM-09151-2, a new potent neuroleptic, to D2-dopaminergic receptors

Jpn J Pharmacol. 1983 Aug;33(4):749-55. doi: 10.1254/jjp.33.749.

Abstract

Effects of YM-09151-2 and five other neuroleptics (haloperidol, spiperone, chlorpromazine, sulpiride and clozapine) on the binding of [3H]-ligands to nine different receptors (alpha 1-adrenergic, alpha 2-adrenergic, beta-adrenergic, muscarinic, D2-dopaminergic, H1-histaminergic, 5HT1-serotonergic, 5HT2-serotonergic and opiate receptors) and on dopamine-sensitive adenylate cyclase were determined using brain membranes in the rat, guinea-pig and dog. The affinity of YM-09151-2 for D2-receptors with a Ki value of 0.1 nM was more than 1000-times higher than that for the other receptors and dopamine-sensitive adenylate cyclase, and it was the greatest among the neuroleptics tested.

MeSH terms

  • Adenylyl Cyclases / metabolism
  • Animals
  • Antipsychotic Agents / metabolism*
  • Benzamides / metabolism*
  • Guinea Pigs
  • In Vitro Techniques
  • Kinetics
  • Male
  • Membranes / metabolism
  • Proteins / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / metabolism*
  • Spiperone / metabolism

Substances

  • Antipsychotic Agents
  • Benzamides
  • Proteins
  • Receptors, Dopamine
  • Spiperone
  • Adenylyl Cyclases
  • nemonapride