Abstract
The human thromboxane A2 receptor (TXA2-R)-coding gene was introduced into Chinese hamster ovary cells and a cell line (TCHO-25) stably expressing TXA2-R, at a level of 3 x 10(5)/cell, was obtained. An anti-asthmatic agent AA-2414 [(+-)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7- phenylheptanoic acid] competitively inhibited the specific binding of a TXA2 mimic ([3H]U-46619) to the TCHO-25 cells, with an IC50 of 6.0 x 10(-8) M, indicating that the drug is an antagonist of human TXA2-R. The TCHO-25 cells offer a tool for the screening and characterization of human TXA2-R antagonists.
MeSH terms
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15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
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Animals
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Asthma / drug therapy*
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Benzoquinones / pharmacology*
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Binding, Competitive / drug effects
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CHO Cells
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Cloning, Molecular
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Cricetinae
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Guinea Pigs
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Heptanoic Acids / pharmacology*
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Humans
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In Vitro Techniques
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Plasmids
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Prostaglandin Endoperoxides, Synthetic / pharmacokinetics
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Receptors, Thromboxane / antagonists & inhibitors*
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Receptors, Thromboxane / biosynthesis
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Receptors, Thromboxane / genetics
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Thromboxane A2 / analogs & derivatives
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Thromboxane A2 / pharmacokinetics
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Trachea / drug effects
Substances
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Benzoquinones
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Heptanoic Acids
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Prostaglandin Endoperoxides, Synthetic
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Receptors, Thromboxane
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seratrodast
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Thromboxane A2
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15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid