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

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

doi:10.1016/0090-6980(87)90107-9

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

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

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

40 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 K_d of 11 ± 4 nM (n=4). Scatchard analysis of equilibrium binding studies revealed one class of high affinity binding sites with a K_d of 20 ± 7nM and a B_max 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 K_ds 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 language	English
Pages (from-to)	789-797
Number of pages	9
Journal	Prostaglandins
Volume	33
Issue number	6
DOIs	https://doi.org/10.1016/0090-6980(87)90107-9
State	Published - 1 Jan 1987
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Endocrinology

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

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.",

author = "Noah Liel and Mais, {Dale E.} and Halushka, {Perry V.}",

note = "Funding Information: Supported in part by HL36838, HL29566 end RR1070. Dr. Lisl is an UpJohn Postdoctoral Cllnlcal Pharmacology Fellow. Dr. Hslushka is a Burroushs-Wellcome Scholar in Cllnlcal Pharmacology.",

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doi = "10.1016/0090-6980(87)90107-9",

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AU - Mais, Dale E.

AU - Halushka, Perry V.

N1 - Funding Information: Supported in part by HL36838, HL29566 end RR1070. Dr. Lisl is an UpJohn Postdoctoral Cllnlcal Pharmacology Fellow. Dr. Hslushka is a Burroushs-Wellcome Scholar in Cllnlcal Pharmacology.

PY - 1987/1/1

Y1 - 1987/1/1

N2 - 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.

AB - 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.

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JF - Prostaglandins

IS - 6

ER -

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

Abstract

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