Interaction of flunarizine with dopamine D2 and D1 receptors

Eur J Pharmacol. 1991 May 17;197(2-3):221-3. doi: 10.1016/0014-2999(91)90526-v.

Abstract

Flunarizine dose dependently inhibits the binding of both [3H]spiperone and [3H]SCH 23390 with Ki values of 112 +/- 9 and 532 +/- 39 nM, respectively. The inhibition of [3H]spiperone binding by flunarizine was competitive as revealed by the Schild plot. The results indicate that flunarizine is a fairly potent dopamine D2 receptor antagonist and offer a possible explanation for the extrapyramidal side-effects observed in patients treated with the drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzazepines / metabolism
  • Binding, Competitive
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism
  • Flunarizine / metabolism
  • Flunarizine / pharmacology*
  • In Vitro Techniques
  • Kinetics
  • Male
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine / metabolism
  • Receptors, Dopamine D1
  • Receptors, Dopamine D2
  • Spiperone / metabolism

Substances

  • Benzazepines
  • Receptors, Dopamine
  • Receptors, Dopamine D1
  • Receptors, Dopamine D2
  • Spiperone
  • Flunarizine