Kuz'mitskiĭ B B, Malaeva L P, Khlevnikova T S, Lakhvich F A
Farmakol Toksikol. 1989 Jul-Aug;52(4):45-8.
The effects of 11 new analogues of 7-aza- and 13-azaprostanoic acid on platelet aggregation of the rat were studied in vitro and ex vivo. The analogues of 13-azaprostanoic acid in vitro (10(-7)-10(-8) mol/l) were found to exhibit the antiaggregation activity in the blood. The compounds containing five-member cycle are more active antiaggregants. They decrease by 70-80% the degree of platelet aggregation stimulated by thrombin and ADP. The modification of omega-chain of these analogues (alkyl, phenyl) exerts no effect on the antiaggregation activity. The antiaggregation action of these compounds in ex vivo condition (5-10 micrograms/kg) does not preserve. 7-azaprostanoids possess the proaggregation activity in vitro.
研究了11种新的7-氮杂和13-氮杂前列腺酸类似物对大鼠血小板聚集的体内外作用。发现13-氮杂前列腺酸类似物在体外（10⁻⁷ - 10⁻⁸mol/l）对血液表现出抗聚集活性。含五元环的化合物是更具活性的抗聚集剂。它们可使凝血酶和ADP刺激的血小板聚集程度降低70 - 80%。这些类似物ω链（烷基、苯基）的修饰对其抗聚集活性无影响。这些化合物在体内条件下（5 - 10微克/千克）的抗聚集作用不能维持。7-氮杂前列腺素在体外具有促聚集活性。
