Assessment of binding indices and physiological responsiveness of the 5-HT2 receptor on human platelets

P. Anne McBride, J. John Mann, Margaret J. Polley, Amy J. Wiley, John A. Sweeney

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54 Scopus citations

Abstract

This is the first report of parallel studies of binding indices and physiological responsiveness of the "Serotonin-two" (5-HT2) receptor on the human platelet membrane. Binding indices were measured by a microassay employing [125I] ILSD as radioligand and ketanserin to define specific binding. A single receptor population was found, characterized by a KD of 1.69 ± 0.45 nM and Bmax of 14.5 ± 6.0 pmol/g protein in healty subjects. Functioning responsiveness of the platelet 5-HT2 receptor complex was assessed by measurement induced by threshold concentrations of adenosine diphosphate (ADP). A statistically significant positive correlation was found between the number of platelet 5-HT2 receptor sites (Bmax) and the magnitude of the serotonin-amplified aggregation response (r = 70, n = 38, p<0.001). Assessment 5-HT2 receptor complex should facilitate study of of the platelet 5-HT2 receptor complex should facilitate study of age, hormonal, disease, and drug effects on 5-HT2 receptor function in human subjects.

Original languageEnglish (US)
Pages (from-to)1799-1809
Number of pages11
JournalLife Sciences
Volume40
Issue number18
DOIs
StatePublished - May 4 1987

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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    Anne McBride, P., John Mann, J., Polley, M. J., Wiley, A. J., & Sweeney, J. A. (1987). Assessment of binding indices and physiological responsiveness of the 5-HT2 receptor on human platelets. Life Sciences, 40(18), 1799-1809. https://doi.org/10.1016/0024-3205(87)90091-9