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一类新型长效血小板活化因子受体拮抗剂的合成与药理学研究

Synthesis and pharmacology of a novel class of long-lasting PAF receptor antagonists.

作者信息

Houlihan W J, Cheon S H, Handley D A, Larson D A

机构信息

Sandoz Research Institute, East Hanover, NJ 07936.

出版信息

J Lipid Mediat. 1991 Jan-Feb;3(1):91-9.

PMID:1662991
Abstract

Several new charged PAF receptor antagonists were prepared, where the phosphate moiety has been replaced by a methylsulfonylcarbamoylpyridinium moiety, and evaluated for duration of inhibitory activity against PAF-induced bronchoconstriction and hemoconcentration in the guinea pig. One of these compounds (1d; SDZ 64-619) has shown potency and duration of inhibition in the range of CV-6209 (1c).

摘要

制备了几种新的带电荷的血小板活化因子(PAF)受体拮抗剂,其中磷酸部分已被甲基磺酰氨基甲酰吡啶鎓部分取代,并评估了它们对豚鼠PAF诱导的支气管收缩和血液浓缩的抑制活性持续时间。这些化合物之一(1d;SDZ 64-619)在抑制效力和持续时间方面与CV-6209(1c)相当。

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