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 3×105/cell, was obtained. An anti-asthmatic agent AA-2414 [(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid]...

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Veröffentlicht in:	Biological & pharmaceutical bulletin 1994/03/15, Vol.17(3), pp.383-385
Hauptverfasser:	KUROKAWA, Tomofumi, MATSUMOTO, Tatsumi, ASHIDA, Yasuko, SASADA, Reiko, IWASA, Susumu
Format:	Artikel
Sprache:	eng
Schlagworte:	(±)-7-(3, 5, 6-trimethyl-1, 4-benzoquinon-2-yl)-7-phenylheptanoic acid 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid AA-2414 Animals anti-asthmatic agent Asthma - drug therapy Benzoquinones - pharmacology Binding, Competitive - drug effects Biological and medical sciences CHO Cells Cloning, Molecular Cricetinae Guinea Pigs Heptanoic Acids - pharmacology Humans In Vitro Techniques Medical sciences Muscle Contraction - drug effects Muscle, Smooth - drug effects Pharmacology. Drug treatments Plasmids Prostaglandin Endoperoxides, Synthetic - pharmacokinetics Receptors, Thromboxane - antagonists & inhibitors Receptors, Thromboxane - biosynthesis Receptors, Thromboxane - genetics Respiratory system Thromboxane A2 - analogs & derivatives Thromboxane A2 - pharmacokinetics thromboxane A2 receptor antagonist Trachea - drug effects
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Zusammenfassung:	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 3×105/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 6.0×10-8M, 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.
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.17.383