BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes
References (26)
- et al.
A new structural analogue antagonist of peptido-leukotrienes. The discovery of BAY x7195
Bioorg. Med. Chem. Letts.
(1993) - et al.
Evidence for two leukotriene receptor subtypes in the guinea-pig isolated ileum
Eur. J. Pharmacol.
(1990) - et al.
Characterisation of the peptido-leukotriene receptor PL2 on the ferret spleen strip
Eur. J. Pharmacol.
(1993) - et al.
Leukotriene-C4 enhances mucus production from submucosal glands in canine trachea in vivo
Int. J. Immunopharmacol.
(1983) - et al.
The inhibition of [3H] leukotriene D4 binding to guinea-pig lung membranes. The correlation of binding affinity with activity on the guinea-pig ileum
Eur. J. Pharmacol.
(1990) - et al.
The effect of leukotrienes C4 and D4 on the microvasculature of guinea-pig skin
Prostaglandins
(1981) - et al.
Introduction of a nomenclature: leukotrienes
Prostaglandins
(1979) - et al.
Pharmacology of peptide leukotrienes on ferret isolated airway smooth muscle
Prostaglandins
(1986) - et al.
Some quantitative uses of drug antagonists
Br. J. Pharmacol. Chemother.
(1959) - et al.
Pharmacological evidence that human intralobar airways do not contain different receptors that mediate contractions to leukotriene C4 and leukotriene D4
J. Pharmacol. Exp. Ther.
(1986)
The role of leukotriene antagonists and inhibitors in the treatment of airway disease
Am. Rev. Resp. Dis.
Relationship between the inhibition constant (Ki) and the concentration of inhibitor which causes 50 per cent inhibition (IC50) of an enzymatic reaction
Biochem. Pharmacol.
The spirally cut tracheal strip preparation
J. Pharm. Pharmacol.
Cited by (74)
Potential role of leukotriene receptor antagonists in reducing cardiovascular and cerbrovascular risk: A systematic review of human clinical trials and in vivo animal studies
2018, Biomedicine and PharmacotherapyCitation Excerpt :CysLT1R and CysLT2R are the two G-protein coupled receptors of the CysLTs [3] that are found in injured human arteries [4,5]. Montelukast, zafirlukast, pranlukast and pobilukast were the first leukotriene receptor antagonists (LTRA) and selective inhibitors of CysLT1 receptor that were approved for use in asthmatic patients [6,7], and later on for the treatment of allergic rhinitis and urticaria [8]. In experimental models (in vivo), they have demonstrated to play a role in reducing the blood-brain barrier permeability and brain injuries [9–12].
Leukotriene C<inf>4</inf> induces bronchoconstriction and airway vascular hyperpermeability via the cysteinyl leukotriene receptor 2 in S-hexyl glutathione-treated guinea pigs
2015, European Journal of PharmacologyCitation Excerpt :As LTD4 is known to activate both human CysLT1 and CysLT2 receptors, it would be interesting to see if both CysLT1 and CysLT2 receptors are involved in human bronchoconstriction. It has been shown that a CysLT1 receptor antagonist does not completely inhibit tracheal contraction induced by high concentrations of LTD4 and that residual contraction to LTD4 is inhibited by the CysLT1/LT2 receptor antagonist BAY u9773 (Bäck et al., 2001; Tudhope et al., 1994). In addition to bronchoconstriction, CysLTs also induce potent airway vascular hyperpermeability (Nakagawa et al., 1992).
The role of leukotrienes in allergic diseases
2015, Allergology InternationalCitation Excerpt :CysLT1 is sensitive to classical antagonists such as montelukast, zafirlukast, pranlukast, pobilukast, and MK571, whereas CysLT2 mediates several effects that are not inhibited by classical antagonists.129 One compound, BAYu9773, antagonizes both CysLT1 and CysLT2 receptors; however, it is neither potent nor selective for these CysLT receptors, especially in human tissues.130 A recent report suggests that BAYu9773 partially agonizes CysLT2.131
Endothelial Cysteinyl Leukotriene 2 Receptor Expression and Myocardial Ischemia/Reperfusion Injury
2008, Trends in Cardiovascular Medicine