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新型具有抗血小板活性的脑血管扩张剂3-异丁酰基-2-异丙基吡唑并-[1,5a]-吡啶(KC-404)对前列环素诱导的大鼠血小板中环磷酸腺苷含量增加的增强作用。

Potentiating effect of 3-isobutyryl-2-isopropylpyrazolo-[1,5a]-pyridine (KC-404), a new cerebral vasodilator with anti-platelet activity, on prostacyclin-induced increase of cyclic AMP content in platelets of rat.

作者信息

Hisayama T, Takayanagi I, Goromaru N, Okamoto Y

机构信息

Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences, Chiba, Japan.

出版信息

Gen Pharmacol. 1989;20(2):183-6. doi: 10.1016/0306-3623(89)90012-8.

Abstract
  1. The effect of KC-404, a new antiplatelet and cerebrovasodilating drug, on prostacyclin (PGI2)-induced accumulation of cyclic AMP was investigated using washed platelets of rat. 2. PGI2 enhanced the cyclic AMP content in a concentration-dependent manner. 3. KC-404 at a relatively high concentrations (above 4.34 microM) significantly increased the maximum cyclic AMP accumulation induced by PGI2, without change in its sensitivity. 4. It is concluded that KC-404 potentiates a mechanism of action of PGI2, and a possible relevance of KC-404 for the treatment of cerebrovascular disorders with a tendency of accompanying thromboembolism is suggested.
摘要
  1. 使用大鼠洗涤血小板研究了新型抗血小板和脑血管舒张药物KC-404对前列环素(PGI2)诱导的环磷酸腺苷(cAMP)积累的影响。2. PGI2以浓度依赖性方式提高cAMP含量。3. 相对高浓度(高于4.34微摩尔)的KC-404显著增加PGI2诱导的最大cAMP积累,而其敏感性无变化。4. 得出结论,KC-404增强PGI2的作用机制,并提示KC-404对于治疗伴有血栓栓塞倾向的脑血管疾病可能具有相关性。

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