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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Bibliographic Details
Published inBiological & pharmaceutical bulletin Vol. 17; no. 3; pp. 383 - 385
Main Authors KUROKAWA, Tomofumi, MATSUMOTO, Tatsumi, ASHIDA, Yasuko, SASADA, Reiko, IWASA, Susumu
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1994
Maruzen
Japan Science and Technology Agency
Subjects
(±)-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
Human
Thromboxane A2
Antagonist
Antiasthma agent
Mechanism of action
In vitro
Biological receptor
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Summary: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.
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ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.17.383