Binding of a thromboxane A2/prostaglandin H2 agonist [3H]U46619 to washed human platelets

Noah Liel, Dale E. Mais, Perry V. Halushka

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39 Scopus citations

Abstract

The binding characteristics of [3H]U46619 to washed human platelets were studied. [3H]U46619 binding to washed human platelets was saturable and displaceable. Kinetic studies yielded a Kd of 11 ± 4 nM (n=4). Scatchard analysis of equilibrium binding studies revealed one class of high affinity binding sites with a Kd of 20 ± 7nM and a Bmax of 9.1 ± 2.3 fmole/107 platelets (550 ± 141 binding sites per platelet) (n=4). A number of compounds that act as either agonists or antagonists of the TXA2/PGH2 receptor were tested for their ability to inhibit the binding of [3H]U46619 to washed human platelets. The Kds of the agonists and antagonists were similar to their potencies to induce or inhibit platelet aggregation. These data provide some evidence that [3H]U46619 binds to the putative human platelet TXA2/PGH2 receptor.

Original languageEnglish
Pages (from-to)789-797
Number of pages9
JournalProstaglandins
Volume33
Issue number6
DOIs
StatePublished - 1 Jan 1987
Externally publishedYes

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