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Antagonism of the Human Thromboxane A2 Receptor by an Anti-asthmatic Agent AA-2414
- Source :
- Biological and Pharmaceutical Bulletin. 17:383-385
- Publication Year :
- 1994
- Publisher :
- Pharmaceutical Society of Japan, 1994.
-
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.
- Subjects :
- Guinea Pigs
Receptors, Thromboxane
Cell
Pharmaceutical Science
CHO Cells
In Vitro Techniques
Pharmacology
Binding, Competitive
Thromboxane receptor
Thromboxane A2
chemistry.chemical_compound
Cricetinae
Benzoquinones
medicine
Animals
Humans
Cloning, Molecular
Chemistry
Chinese hamster ovary cell
Muscle, Smooth
General Medicine
Seratrodast
Asthma
Prostaglandin Endoperoxides, Synthetic
Trachea
medicine.anatomical_structure
Mechanism of action
Heptanoic Acids
Cell culture
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
lipids (amino acids, peptides, and proteins)
medicine.symptom
Antagonism
Muscle Contraction
Plasmids
circulatory and respiratory physiology
Subjects
Details
- ISSN :
- 13475215 and 09186158
- Volume :
- 17
- Database :
- OpenAIRE
- Journal :
- Biological and Pharmaceutical Bulletin
- Accession number :
- edsair.doi.dedup.....ed8ba7d91321857a6756e3f339f51160