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Selective CysLT1 leukotriene receptor antagonist.
Prod. No. S 7690
Leukotrienes exist as two distinct classes, hydroxyacids such as LTB4 (Prod. No.
L 0517), and cysteinyl leukotrienes such as LTC4 (Prod. No. L 4886), LTD4 (Prod. No. L 5011) and LTE4. Recently cloned leukotriene receptors BLT1, CysLT1 and CysLT2 are members of the G protein-coupled receptor superfamily. Cysteinyl leukotrienes are important mediators of inflammatory responses, such as
constriction of airways and vascular smooth muscle, increased endothelial membrane permeability leading to edema, and an enhanced secretion of viscous mucus. Their receptors have been implicated in a range of inflammatory diseases, specifically bronchial asthma. SR2640 acts as a selective CysLT1 leukotriene receptor antagonist.
- Inhibits in a concentration-dependent manner the binding of 0.4 nM [3H]LTD4 to guinea pig lung
membrane with an
IC50 value of 23 nM resulting in inhibition of bronchoconstriction.1
- Inhibits LTD4-stimulated increases in intracellular calcium and production of inositol phosphates in human
polymorphonuclear neutrophils (PMN).3
- In an in vivo model of chronic inflammatory bowel disease, SR2640 reduces inhibitory effects of
LTD4 on LTB4-directed
chemotaxis of PMN neutrophils by acting as systemic LTD4 receptor antagonist.4
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References:
- Ahnfelt-Ronne, I., et al., Eur. J. Pharmacol., 155, 117-128 (1988).
- Bouchelouche, P.N., et al., Agents and Actions, 29, 1990, 299-307 (1990).
- Nielsen, O.H., et al., Prostaglandins Leukot. Essent. Fatty Acids, 42, 181-184 (1991).
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