Binding of an [125I] labelled thromboxane A2/prostaglandin H2 receptor agonist to baboon platelets

G. W. Dorn; A. De Jesus

doi:10.1016/0090-6980(89)90047-6

Binding of an [¹²⁵I] labelled thromboxane A₂/prostaglandin H₂ receptor agonist to baboon platelets

G. W. Dorn, A. De Jesus

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

3 Scopus citations

Abstract

To characterize the thromboxane A₂/prostaglandin H₂ (TXA₂/PGH₂) receptor on baboon platelets the binding of [¹²⁵I]BOP was studied. [¹²⁵I]BOP bound to washed baboon platelets in a saturable manner. Scatchard analysis of binding isotherms revealed a K_d of 1.12 ± 0.08 nM and a binding capacity of 54 ± 5 fmoles/10⁹ platelets (326 sites/platelet). Several TXA₂/PGH₂ agonists and antagonists displaced [¹²⁵I]BOP from its baboon platelet binding site with a rank order of potency similar to human platelets: I-BOP > SQ29548 > U46619 = I-PTA-OH. I-BOP aggregated washed baboon platelets with an EC₅₀ of 10 ± 4 nM. The results indicate that [¹²⁵I]BOP binds to the TXA₂/PGH₂ receptor on baboon platelets and that this receptor is similar to its human conterpart.

Original language	English
Pages (from-to)	645-653
Number of pages	9
Journal	Prostaglandins
Volume	38
Issue number	6
DOIs	https://doi.org/10.1016/0090-6980(89)90047-6
State	Published - Dec 1989

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title = "Binding of an [125I] labelled thromboxane A2/prostaglandin H2 receptor agonist to baboon platelets",

abstract = "To characterize the thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor on baboon platelets the binding of [125I]BOP was studied. [125I]BOP bound to washed baboon platelets in a saturable manner. Scatchard analysis of binding isotherms revealed a Kd of 1.12 ± 0.08 nM and a binding capacity of 54 ± 5 fmoles/109 platelets (326 sites/platelet). Several TXA2/PGH2 agonists and antagonists displaced [125I]BOP from its baboon platelet binding site with a rank order of potency similar to human platelets: I-BOP > SQ29548 > U46619 = I-PTA-OH. I-BOP aggregated washed baboon platelets with an EC50 of 10 ± 4 nM. The results indicate that [125I]BOP binds to the TXA2/PGH2 receptor on baboon platelets and that this receptor is similar to its human conterpart.",

author = "Dorn, {G. W.} and {De Jesus}, A.",

note = "Funding Information: The authors wish to thank Hilda Johnson for her secretarial assistance and Richard A. Walsh, M.D. for the opportunity to obtain baboon platelets. Supported by grants from the Veterans Administration, the American Heart Association, Texas Affiliate, and the National Heart, Lung and Blood Institute of the National Institute of Health (HL-33579).",

year = "1989",

month = dec,

doi = "10.1016/0090-6980(89)90047-6",

language = "English",

volume = "38",

pages = "645--653",

journal = "Prostaglandins",

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T1 - Binding of an [125I] labelled thromboxane A2/prostaglandin H2 receptor agonist to baboon platelets

AU - Dorn, G. W.

AU - De Jesus, A.

N1 - Funding Information: The authors wish to thank Hilda Johnson for her secretarial assistance and Richard A. Walsh, M.D. for the opportunity to obtain baboon platelets. Supported by grants from the Veterans Administration, the American Heart Association, Texas Affiliate, and the National Heart, Lung and Blood Institute of the National Institute of Health (HL-33579).

PY - 1989/12

Y1 - 1989/12

N2 - To characterize the thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor on baboon platelets the binding of [125I]BOP was studied. [125I]BOP bound to washed baboon platelets in a saturable manner. Scatchard analysis of binding isotherms revealed a Kd of 1.12 ± 0.08 nM and a binding capacity of 54 ± 5 fmoles/109 platelets (326 sites/platelet). Several TXA2/PGH2 agonists and antagonists displaced [125I]BOP from its baboon platelet binding site with a rank order of potency similar to human platelets: I-BOP > SQ29548 > U46619 = I-PTA-OH. I-BOP aggregated washed baboon platelets with an EC50 of 10 ± 4 nM. The results indicate that [125I]BOP binds to the TXA2/PGH2 receptor on baboon platelets and that this receptor is similar to its human conterpart.

AB - To characterize the thromboxane A2/prostaglandin H2 (TXA2/PGH2) receptor on baboon platelets the binding of [125I]BOP was studied. [125I]BOP bound to washed baboon platelets in a saturable manner. Scatchard analysis of binding isotherms revealed a Kd of 1.12 ± 0.08 nM and a binding capacity of 54 ± 5 fmoles/109 platelets (326 sites/platelet). Several TXA2/PGH2 agonists and antagonists displaced [125I]BOP from its baboon platelet binding site with a rank order of potency similar to human platelets: I-BOP > SQ29548 > U46619 = I-PTA-OH. I-BOP aggregated washed baboon platelets with an EC50 of 10 ± 4 nM. The results indicate that [125I]BOP binds to the TXA2/PGH2 receptor on baboon platelets and that this receptor is similar to its human conterpart.

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DO - 10.1016/0090-6980(89)90047-6

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SN - 0090-6980

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JO - Prostaglandins

JF - Prostaglandins

IS - 6

ER -

Binding of an [¹²⁵I] labelled thromboxane A₂/prostaglandin H₂ receptor agonist to baboon platelets

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