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Quinotolast sodium

CAS No. : 101193-62-8

MCE 站：Quinotolast sodium

产品活性：Quinotolast sodium (浓度范围为 1-100 μg/mL) 抑制组胺，LTC₄ 和 PGD₂ 释放，这种作用具有浓度依赖性。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor  |  Leukotriene Receptor  |  Prostaglandin Receptor

In Vitro: Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C₄ and prostaglandin (PG) D₂ from dispersed human lung cells. Quinotolast (100 μg/mL) significantly inhibits PGD₂ and LTC₄ release. Quinotolast inhibits PGD₂ release by 100% and LTC₄ release by 54%. The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period, no tachyphylaxis being observed. Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells. Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells. The IC₅₀ value for Quinotolast is 0.72 μg/mL.

In Vivo: Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. When Quinotolast is given i.v. to rats, Quinotolast, dose-dependently inhibits PCA. The doses of Quinotolast required to inhibit the reaction by 50% (ED₅₀) is 0.0063 mg/kg. Given p.o., Quinotolast inhibits the reaction. ED₅₀ value for Quinotolast is 0.0081 mg/kg. Although almost complete inhibition is observed with Quinotolast at a dose of 0.32 mg/kg, its effect is slightly attenuated at a dose of 1 mg/kg.

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