蒎烷血栓素A2衍生物的抗血栓素A2作用
Anti-thromboxane A2 actions of pinane thromboxane A2 derivatives.
作者信息
Roth D M, Lefer A M, Smith J B, Nicolaou K C
出版信息
Prostaglandins Leukot Med. 1982 Nov;9(5):503-9. doi: 10.1016/0262-1746(82)90031-2.
Six pinane-thromboxane A2 analogs have been synthesized and tested for their ability to antagonize carbocyclic thromboxane A2 (CTA2) induced coronary vasoconstriction and prostaglandin endoperoxide analog induced platelet aggregation. Two of the derivatives, 5C-15S BPTA2 and 5T-15S BPTA2 and 5T-15S BPTA2 (1 microM) showed 76 +/- 3 and 72 +/- 9 percent inhibition of CTA2 (15 nM) induced vasoconstriction of cat coronary arteries respectively, while the other compounds showed between 15 and 50 percent inhibition at 1.0 and 2.0 microM. 5C-15S BPTA2 also antagonized prostaglandin-endoperoxide analog induced human platelet aggregation, although the other compounds showed little or no antagonism of aggregation in this system.
已合成六种蒎烷 - 血栓素A2类似物，并测试了它们拮抗环戊烷血栓素A2（CTA2）诱导的冠状动脉收缩和前列腺素内过氧化物类似物诱导的血小板聚集的能力。其中两种衍生物，5C - 15S BPTA2和5T - 15S BPTA2（1微摩尔）分别对CTA2（15纳摩尔）诱导的猫冠状动脉收缩表现出76±3%和72±9%的抑制作用，而其他化合物在1.0和2.0微摩尔时表现出15%至50%的抑制作用。5C - 15S BPTA2也拮抗前列腺素内过氧化物类似物诱导的人血小板聚集，尽管其他化合物在该系统中对聚集几乎没有或没有拮抗作用。
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