The cysteinyl-leukotriene receptor antagonist BAY u9773 is a competitive antagonist of leukotriene C4 in the guinea-pig ileum

European Journal of Pharmacology
M BäckS E Dahlén

Abstract

Two main classes of receptors exist for leukotrienes C4, D4 and E4, collectively named cysteinyl-leukotrienes (CysLTs). The CysLT1 receptor is blocked by currently available leukotriene antagonists, and the CysLT2 receptor is defined by the absence of selective antagonists. The contractile response to leukotriene C4 in guinea-pig ileum longitudinal muscle is resistant to CysLT1 receptor antagonists. However, the leukotriene E4 analogue BAY u9773 (6(R)-(4'-carboxyphenylthio)-5(S)-hydroxy-7(E),9(E),11(Z), 14(Z)-eicosatetraenoic acid) has recently been reported to inhibit CysLT2 responses. Therefore BAY u9773 was evaluated for antagonism of the effect of leukotriene C4 in the guinea-pig ileum longitudinal muscle. We found that BAY u9773 (0.3-10 microM) did not contract the preparation, but produced a concentration-dependent rightward shift in the concentration-response relation for leukotriene C4. Schild plot analysis yielded a slope which was not significantly different from unity and a pA2 value of 6.1. The inhibition of leukotriene C4 by BAY u9773 was not altered by antagonism of CysLT1 receptors by ICI 198,615 {[1-[[2-methoxy-4-[[(phenylsulfonyl)amino]carbonyl]-phenyl] methyl]-1H-indazol-6-yl]carbamic acid cyclopentyl ester}(1...Continue Reading

References

Jul 3, 1990·European Journal of Pharmacology·P J GardinerN J Cuthbert
Oct 17, 1973·Nature: New Biology·J AugsteinM L Tattersall
Nov 1, 1980·Proceedings of the National Academy of Sciences of the United States of America·D E SokC J Sih
Feb 1, 1983·Prostaglandins·R D KrellR E Giles
Nov 3, 1994·European Journal of Pharmacology·S R TudhopeP J Gardiner
Jul 6, 1993·European Journal of Pharmacology·P J GardinerT S Abram
Nov 1, 1995·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·B Dahlén, S E Dahlén
Mar 1, 1959·British Journal of Pharmacology and Chemotherapy·O ARUNLAKSHANA, H O SCHILD
Apr 1, 1964·British Journal of Pharmacology and Chemotherapy·H P RANG

❮ Previous
Next ❯

Citations

Aug 7, 1999·Clinical Reviews in Allergy & Immunology·S E Dahlén
Aug 11, 2000·European Journal of Pharmacology·M BäckC Brink
Dec 31, 2002·European Journal of Pharmacology·Sumei LiuJackie D Wood
Oct 31, 1998·European Journal of Pharmacology·E Wikström JonssonS E Dahlén
Feb 15, 2000·American Journal of Respiratory and Critical Care Medicine·S E Dahlén
Jul 23, 2015·Journal of Medicinal Chemistry·Satoshi ItadaniKazuyuki Ohmoto
Jul 25, 2008·Neurogastroenterology and Motility : the Official Journal of the European Gastrointestinal Motility Society·B-S ChangS-C Huang
Apr 30, 2011·Chemical Reviews·Motonao Nakamura, Takao Shimizu
Nov 20, 2014·ACS Medicinal Chemistry Letters·Satoshi ItadaniJun Takeuchi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.