cyslt2

Gemilukast (ONO-6950) is an orally active and potent dual inhibitor of cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2), inhibits LTC 4-induced bronchoconstriction, and is inhibitory to human CysLT1 and CysLT2, and may be used in the treatment of asthma.

Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively. It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.

HAMI 3379 (HAMI3379) is a selective cysteinyl leukotriene receptor 2 (CysLT2) antagonist that dose- and time-dependently attenuates brain damage and inhibits microglial cell inflammation following focal cerebral ischemia in rats and attenuates ischemia-like neuronal damage by inhibiting microglial activation.

S-Geranylgeranyl-L-glutathione acts as a ligand for the orphan G protein-coupled receptor (GPCR) P2RY8, displaying selective affinity by inducing internalization of P2RY8 in preference to the sphingosine-1-phosphate receptor 2 (S1P2), GPR55, cysteinyl leukotriene receptor 1 (CysLT1 receptor), and the CysLT2 receptor at a concentration of 100 nM. Additionally, at a lower concentration of 10 nM, S-Geranylgeranyl-L-glutathione inhibits the chemokine (C-X-C motif) ligand 12-induced migration of both P2RY8-expressing WEHI-231 B cell lymphoma cells and human tonsil germinal center B cells.

BAY-u 9773 is a non-selective antagonist of cysteinyl leukotrienes receptors (CysLT receptors), with approximately equal IC50 values for both CysLT1 and CysLT2. BAY-u 9773 is used to inhibit leukotriene responses [1].

HAMI 3379 is a potent and selective antagonist of the Cysteinyl leukotriene (CysLT2) receptor. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury. It also attenuates microglia-related inflammation.

ONO-2050297 is the first potent dual CysLT1 and CysLT2 antagonist with IC50 values of 0.017 μM (CysLT1) and 0.00087 μM (CysLT2), respectively.

Quininib is a regulator of Ocular Angiogenesis. Quininib significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice.

ONO-4310321 is a potent, orally available dual CysLT1 and CysLT2 receptor antagonist.