In vitro affinity of piribedil for dopamine D3 receptor subtypes, an autoradiographic study

Alfredo Cagnotto, Luca Parotti, Tiziana Mennini

Research output: Contribution to journalArticle

Abstract

Receptor binding autoradiography, using the selective ligand [3H]7-OH-(R)DPAT (R(+)-2-dipropylamino-7-hydroxy 1,2,3,4-tetrahydronaphthalene), showed that piribedil is a potent inhibitor at dopamine D3 receptors in limbic regions (island of Calleja), with affinity (IC50) between 30 and 60 nM. The in vitro IC50 of piribedil for inhibition of [3H]spiperone binding to receptors of the dopamine D2-like family (D2, D3 and D4), ranged between 10-7 and 10-6 M in different brain regions (medial and lateral caudate putamen, olfactory tubercles, and nucleus accumbens). At the highest concentration tested (10-5 M) piribedil inhibited dopamine D1 receptor binding by 2 than for dopamine D2-like receptors, and very low affinity for the dopamine D1 receptor subtype in rat brain. How this pattern of receptor affinity is related to the pharmacological profile of piribedil deserves further investigation.

Original languageEnglish
Pages (from-to)63-67
Number of pages5
JournalEuropean Journal of Pharmacology
Volume313
Issue number1-2
DOIs
Publication statusPublished - Oct 10 1996

Keywords

  • Autoradiography
  • Dopamine receptor
  • Piribedil

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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