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Several new charged PAF receptor antagonists were prepared, where the phosphate moiety has been replaced by a methylsulfonylcarbamoylpyridinium moiety, and evaluated for duration of inhibitory activity against PAF-induced bronchoconstriction and hemoconcentration in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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