BayCysLT2

Definition

ChEBI: Benzoic acid, 3-[[(3-carboxycyclohexyl)amino]carbonyl]-4-[3-[4-(4-phenoxybutoxy)phenyl]propoxy]- is an organooxygen compound and an organonitrogen compound. It is functionally related to a gamma-amino acid.

Biological Activity

baycyslt2, an isophthalic acid derivative, is a selective and potent cyslt2 receptor antagonist [1].cysteinyl leukotrienes (cyslts) belong to a family of g protein-coupled receptors (gpcrs). the cysteinyl leukotrienes (cyslts) are inflammatory mediators associated with neuronal injury after brain ischemia through the activation of their receptors, cyslt1r and cyslt2r [2].

in vitro

baycyslt2 inhibited radioligand binding of ltd4 to cyslt2 and cyslt1 receptor cell lines with ic50 values of 35 and >10,000 nm, respectively [1]. baycyslt2 reversed ltc4-stimulated perfusion pressure increase and contractility decrease in isolated langendorff-perfused guinea pig hearts in a concentration-dependent manner [1]. baycyslt2 protected astrocytes from ischemic injury [3].

in vivo

baycyslt2 attenuated myocardial infarction damage but also inhibited ltd4-induced evans blue dye leakage in the mouse ear vasculature [4].

References

[1] m. harter, j. erguden, f. wunder, et al. isophtalic acid derivatives. 10/537,623, 1-104 (2006).
[2] takasaki j, kamohara m, matsumoto m, et al. the molecular characterization and tissue distribution of the human cysteinyl leukotriene cyslt 2 receptor[j]. biochemical and biophysical research communications, 2000, 274(2): 316-322.
[3] x. j. huang, w.p. zhang, c.t. li, w.z. shi, s.h. fang, y.b. lu, z. chen, e.q. wei. activation of cyslt receptors induces astrocyte proliferation and death after oxygen–glucose deprivation. glia, 56 (2008), pp. 27–37
[4] n. c. ni, d. yan, l.l. ballantyne, a. barajas-espinosa st, t. amand, d.a. pratt, c.d. funk. a selective cysteinyl leukotriene receptor 2 antagonist blocks myocardial ischemia/reperfusion injury and vascular permeability in mice. j. pharmacol. exp. ther., 339 (2011), pp. 768–778