Usmanova D M, Musaev U N, Efimov V S
Farmakol Toksikol. 1979 Nov-Dec;42(6):628-32.
Antiheparin activity and acute toxicity of a monomer and polymer quaternary ammonium salts obtained on the basis of the alkaloid lupinine were investigated. The monomer was shown to have no antiheparin activity even when administered in high doses. Lupinine polymetakryloyl iodoethylate is a selective heparin antagonist. This activity of polymers is relative to the extent of polymerization. A compound with a molecular weight of 20 000 turned out the most effective in the tested series of ready-made polymers. Acute toxicity of polycations is considerably less than that elicited by the monomer. The effect of heparin complete neutralization is accompanied by transitory thrombocytopenia.
研究了基于生物碱羽扇豆碱获得的单体和聚合物季铵盐的抗肝素活性和急性毒性。结果表明,即使高剂量给药,该单体也没有抗肝素活性。碘化乙基聚甲基丙烯酸羽扇豆碱酯是一种选择性肝素拮抗剂。聚合物的这种活性与聚合程度有关。在测试的一系列现成聚合物中,分子量为20000的化合物最为有效。聚阳离子的急性毒性明显低于单体引起的毒性。肝素完全中和的作用伴有短暂性血小板减少症。