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

doi:10.1016/0024-3205(87)90091-9

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

Research output: Contribution to journal › Article › peer-review

56 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 K_D 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 language	English (US)
Pages (from-to)	1799-1809
Number of pages	11
Journal	Life Sciences
Volume	40
Issue number	18
DOIs	https://doi.org/10.1016/0024-3205(87)90091-9
State	Published - May 4 1987

ASJC Scopus subject areas

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

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10.1016/0024-3205(87)90091-9

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title = "Assessment of binding indices and physiological responsiveness of the 5-HT2 receptor on human platelets",

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.",

author = "{Anne McBride}, P. and {John Mann}, J. and Polley, {Margaret J.} and Wiley, {Amy J.} and Sweeney, {John A.}",

note = "Funding Information: This project was supported in part by BRSG #S07 PR05396, awarded by the Biomedical Research Support Grant Program, Division of Research Resources, National Institutes of Health; the Stallone Fund for Autism Research; and PHS award MH 40210. Dr. McBride is the recipient of a Teacher-Scientist Award from the AndrewW . Mellon Foundation and a Reader's Digest Research Fellowship. Dr. Mann is the recipient of an Irma T. Hirschl Career Scientist Award. Excellent technical assistance was provided by Ms. Amy Wiley, Mr. Brian Barnett, and Mr. John Paturzo.",

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doi = "10.1016/0024-3205(87)90091-9",

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AU - Anne McBride, P.

AU - John Mann, J.

AU - Polley, Margaret J.

AU - Wiley, Amy J.

AU - Sweeney, John A.

N1 - Funding Information: This project was supported in part by BRSG #S07 PR05396, awarded by the Biomedical Research Support Grant Program, Division of Research Resources, National Institutes of Health; the Stallone Fund for Autism Research; and PHS award MH 40210. Dr. McBride is the recipient of a Teacher-Scientist Award from the AndrewW . Mellon Foundation and a Reader's Digest Research Fellowship. Dr. Mann is the recipient of an Irma T. Hirschl Career Scientist Award. Excellent technical assistance was provided by Ms. Amy Wiley, Mr. Brian Barnett, and Mr. John Paturzo.

PY - 1987/5/4

Y1 - 1987/5/4

N2 - 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.

AB - 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.

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

Abstract

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