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
thromboxane A<SUB>2</SUB> receptor antagonist, Guinea Pigs, Receptors, Thromboxane, AA-2414, CHO Cells, In Vitro Techniques, anti-asthmatic agent, Binding, Competitive, Thromboxane A2, Cricetinae, Benzoquinones, Animals, Humans, Cloning, Molecular, Muscle, Smooth, (±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid, Asthma, Prostaglandin Endoperoxides, Synthetic, Trachea, Heptanoic Acids, 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid, Muscle Contraction, Plasmids
thromboxane A<SUB>2</SUB> receptor antagonist, Guinea Pigs, Receptors, Thromboxane, AA-2414, CHO Cells, In Vitro Techniques, anti-asthmatic agent, Binding, Competitive, Thromboxane A2, Cricetinae, Benzoquinones, Animals, Humans, Cloning, Molecular, Muscle, Smooth, (±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid, Asthma, Prostaglandin Endoperoxides, Synthetic, Trachea, Heptanoic Acids, 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid, Muscle Contraction, Plasmids
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).41 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Average influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!