Modipafant (UK-80067)，UK-74505 的对映体，是一种高效、具有口服活性的选择性的血小板活化因子 (PAF) 拮抗剂。Modipafant 展示了大约两倍于 UK-74505 的内在效力。
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505[1][2].
when preincubated with rabbit platelets, the potency of antagonizing PAF induced aggregation increased markedly when preincubation time with Modipafant was increased from 2 min (IC50=5.6 nM) to 60 min (IC50=0.34 nM)[2].
[1]. Kuitert LM, et al. Effect of a novel potent platelet-activating factor antagonist, modipafant, in clinical asthma. Am J Respir Crit Care Med. 1995;151(5):1331-1335.
[2]. Jezequel SG, et al, a new PAF antagonist: pharmacokinetics and disposition in rat, dog and man. Xenobiotica. 1996;26(9):963-975.
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