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REV 5901 is an antagonist of cysteinyl-leukotriene receptors with a Ki value of 0.7 µM for guinea pig lung membranes.1 It is also an inhibitor of rat neutrophil 5-LO with an IC50 value of 0.12 µM.2
1
Van Inwegen, R.G., Khandwala, A., Gordon, R., et al. REV 5901: An orally effective peptidoleukotriene antagonist, detailed biochemical/pharmacological profile. J Pharmacol Exp Ther241117-124(1987).
2
Musser, J.H., Charkraborty, U.R., Sciortino, S., et al. Substituted arylmethyl phenyl ethers. 1. A novel series of 5-lipoxygenase inhibitors and leukotriene antagonists. J Med Chem3096-104(1987).
Van Inwegen, R.G., Khandwala, A., Gordon, R., et al. REV 5901: An orally effective peptidoleukotriene antagonist, detailed biochemical/pharmacological profile. J Pharmacol Exp Ther241117-124(1987).
Musser, J.H., Charkraborty, U.R., Sciortino, S., et al. Substituted arylmethyl phenyl ethers. 1. A novel series of 5-lipoxygenase inhibitors and leukotriene antagonists. J Med Chem3096-104(1987).
Hogaboam, C.M., Donigi-Gale, D., Shoupe, T.S., et al. Platelet-activating factor synthesis by peritoneal mast cells and its inhibition by two quinoline-based compounds. Br J Pharmacol10587-92(1992).