Identification of D1-like dopamine receptors on human blood platelets

Jacques De Keyser, M. De Waele, A. Convents, Guy Ebinger, G. Vauquelin

Research output: Contribution to journalArticle

27 Citations (Scopus)

Abstract

Dopamine is able to inhibit the epinephrine-induced aggregation of human blood platelets, but the mechanism of action has not been elucidated. In this study we report that membranes from human blood platelets possess high affinity, saturable and stereoselective binding sites for the D1 dopamine receptor antagonist (3H) SCH 23390. (3H) SCH 23390 appeared to label a single class of binding sites with a Bmax of 18.6 +/- 1.6 fmol/mg protein and a KD of 0.8 nM. The potencies of different dopaminergic antagonists and agonists in displacing (3H) SCH 23390 from blood platelet membranes were similar to those obtained for striatal membranes. Unlike the classically defined D1 receptors, e.g. those in striatum, the D1 receptor sites on platelets appeared not to be coupled to the adenylate cyclase system, hence the term "D1-like". The D1 agonist SKF 38393 was more potent than dopamine in inhibiting platelet aggregation induced by epinephrine, and the effects of dopamine and SKF 38393 were prevented by SCH 23390. These results suggest that the inhibitory action of dopamine on the epinephrine-induced platelet aggregation is mediated through these D1-like receptors.
Original languageEnglish
Pages (from-to)1797-1806
Number of pages10
JournalLife Sci
Publication statusPublished - 1988

Keywords

  • Adenylate Cyclase/blood
  • Alprostadil/pharmacology
  • Benzazepines/blood/pharmacology
  • Binding
  • Competitive
  • Blood Platelets/drug effects/*metabolism
  • Cell Membrane/metabolism
  • Comparative Study
  • Cyclic AMP/blood
  • Dopamine/blood/pharmacology
  • Dopamine Antagonists
  • Epinephrine/pharmacology
  • GTP-Binding Proteins/blood
  • Human
  • Platelet Aggregation/drug effects
  • Platelet Aggregation Inhibitors/pharmacology
  • Receptors
  • Dopamine/*metabolism
  • Dopamine D1
  • Serotonin/metabolism

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