Antagonism of the Human Thromboxane A2 Receptor by an Anti-asthmatic Agent AA-2414.
Copyright policy )Antagonism of the Human Thromboxane A2 Receptor by an Anti-asthmatic Agent AA-2414.
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.
- Takeda (Japan) Japan
Guinea Pigs, Receptors, Thromboxane, Muscle, Smooth, CHO Cells, In Vitro Techniques, Binding, Competitive, Asthma, Prostaglandin Endoperoxides, Synthetic, Trachea, Thromboxane A2, Heptanoic Acids, 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid, Cricetinae, Benzoquinones, Animals, Humans, Cloning, Molecular, Muscle Contraction, Plasmids
Guinea Pigs, Receptors, Thromboxane, Muscle, Smooth, CHO Cells, In Vitro Techniques, Binding, Competitive, Asthma, Prostaglandin Endoperoxides, Synthetic, Trachea, Thromboxane A2, Heptanoic Acids, 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid, Cricetinae, Benzoquinones, Animals, Humans, Cloning, Molecular, Muscle Contraction, Plasmids
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