Dopamine D2 receptor blockade and antimigraine action of flunarizine

Cephalalgia. 1994 Jun;14(3):235-40. doi: 10.1046/j.1468-2982.1994.014003235.x.

Abstract

We studied in vivo the influence of flunarizine on dopamine D2 receptors and investigated whether dopamine D2 receptor blockade is involved in its antimigraine action. Eleven migraine patients, treated with flunarizine, 10 mg per day, underwent single photon emission computer tomography (SPECT) using [123I] labeled iodobenzamide, a ligand with high affinity and high specificity for D2 receptors. There was a reduction of the dopamine D2 receptor binding potential in all patients compared to age-matched controls. The efficacy of flunarizine in migraine prophylaxis failed to correlate with the degree of the dopamine D2 receptor blockade. The antimigraine action of flunarizine may not involve antidopaminergic mechanisms.

MeSH terms

  • Adult
  • Aged
  • Brain / diagnostic imaging
  • Brain / drug effects
  • Dopamine D2 Receptor Antagonists*
  • Female
  • Flunarizine / adverse effects
  • Flunarizine / therapeutic use*
  • Humans
  • Iodine Radioisotopes
  • Male
  • Middle Aged
  • Migraine Disorders / drug therapy*
  • Migraine Disorders / physiopathology
  • Receptors, Dopamine D2 / physiology
  • Tomography, Emission-Computed, Single-Photon

Substances

  • Dopamine D2 Receptor Antagonists
  • Iodine Radioisotopes
  • Receptors, Dopamine D2
  • Flunarizine