Klöcking H P, Markwardt F
Institute of Pharmacology and Toxicology, Medical School, Erfurt, Germany.
Pharmazie. 1994 Apr;49(4):227-30.
The acute release of tissue-type plasminogen activator t-PA from the vascular endothelium is of decisive importance for the prevention of intravascular fibrin deposits. A dose-dependent t-PA release from the isolated perfused vascular preparations may be induced by mediators (platelet-activating factor, bradykinin, histamine) adrenergic and cholinergic transmitters (isoprenaline, acetylcholine), thrombin, heparin and analogues, and 1-desamino-8-D-arginine-vasopression (DDAVP). Most of the compounds were shown to enhance the t-PA activity also in animal experiments (rats, rabbits, mini pigs). The pharmacologic stimulation of the t-PA release may be convenient for short-term thrombosis, prophylaxis and partial thrombolysis. Presently, this could only be achieved by unfractionated and low molecular weight heparins which have been shown to release t-PA.
血管内皮组织型纤溶酶原激活剂（t-PA）的急性释放对于预防血管内纤维蛋白沉积起着决定性作用。介质（血小板活化因子、缓激肽、组胺）、肾上腺素能和胆碱能递质（异丙肾上腺素、乙酰胆碱）、凝血酶、肝素及其类似物以及1-去氨基-8-D-精氨酸加压素（DDAVP）可诱导从离体灌注血管制剂中呈剂量依赖性释放t-PA。在动物实验（大鼠、兔子、小型猪）中，大多数化合物也显示可增强t-PA活性。t-PA释放的药理刺激可能适用于短期血栓形成的预防和部分溶栓。目前，这只能通过已被证明可释放t-PA的普通肝素和低分子量肝素实现。
