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大鼠血管组织中的前列环素样活性。赖氨酸乙酰水杨酸治疗可产生快速、持久的抑制作用。

Prostacyclin-like activity in rat vascular tissues. Fast, long-lasting inhibition by treatment with lysine acetylsalicylate.

作者信息

Villa S, de Gaetano G

出版信息

Prostaglandins. 1977;14(6):1117-24. doi: 10.1016/0090-6980(77)90289-1.

Abstract

Both arterial and venous tissues obtained from normal rats released prostacyclin (PGI2)-like activity, as marked by its potent inhibitory effect on platelet aggregation. Intraperitoneal or intravenous administration of a single dose of a soluble lysine salt of acetylsalicyclic acid (L-ASA, 1-400 mg/kg) resulted in abolition or substantial reduction of prostacyclin-like activity released from rat vasculature. The inhibitory effect of L-ASA was evident one minute after its i.v. administration to the animals, persisted for at least 24 hours and was still detectable (in venous tissues only) 168 hours later. Venous tissues were inhibited by doses of L-ASA as low as 1 mg/kg, whereas arterial tissues were not inhibited by doses of LA-ASA lower than 10 mg/kg. This difference may possibly be related to the lower prostacyclin-like activity shown by rat venous tissues compared to arterial ones. It is suggested that L-ASA or part of its molecule may bind to and inhibit cyclo-oxygenase in the blood vessel wall in a manner similar to the acetylation of platelt cyclo-oxygenase.

摘要

从正常大鼠获取的动脉组织和静脉组织均可释放出类似前列环素(PGI2)的活性物质,其对血小板聚集具有显著的抑制作用,以此作为该活性物质的标志。腹腔注射或静脉注射单剂量的乙酰水杨酸赖氨酸盐(L-ASA,1 - 400毫克/千克)会导致大鼠脉管系统释放的类似前列环素的活性物质被消除或大幅减少。对动物静脉注射L-ASA一分钟后,其抑制作用就很明显,持续至少24小时,且在168小时后仍可检测到(仅在静脉组织中)。低至1毫克/千克的L-ASA剂量即可抑制静脉组织,而低于10毫克/千克的L-ASA剂量对动脉组织则无抑制作用。这种差异可能与大鼠静脉组织相比动脉组织显示出的较低的类似前列环素活性有关。有人提出,L-ASA或其分子的一部分可能以类似于血小板环氧化酶乙酰化的方式与血管壁中的环氧化酶结合并抑制它。

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