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CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively[1]. | [in vivo]
In vivo, CP-96021 inhibits iv LTD4- and iv PAF-induced bronchoconstriction in guinea pigs with ED50s of 0.46 and 0.16 mg/kg p.o. respectively. CP-96021 effectively blocks the combined airway obstructive effects of endogenously released PAF and LTD4 stimulated by aerosolized antigen challenge in guinea pigs with an ED50s of 1.8 mg/kg p.o[1]. | [IC 50]
LTC4: 34 nM (Ki); Platelet activating factor (PAF) receptor: 37 nM (Ki) | [References]
[1] A. Marfat, et al. The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 1995, 5 (13): 1377-1382. |
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