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Metabolism of a New Antiaggregant, Indolinone Derivative
Bulletin of Experimental Biology and Medicine ( IF 0.9 ) Pub Date : 2020-04-01 , DOI: 10.1007/s10517-020-04792-y
V V Bykov 1, 2 , K A Leonov 2 , V Yu Serebrov 1 , G A Chernysheva 3 , V I Smol'yakova 3 , M A Solov'ev 3, 4 , E V Udut 1 , V P Fisenko 5 , V V Udut 3, 4
Affiliation  

Cytochrome p450-mediated metabolism of GRS (indolinone antiaggregant) and its effects on activities of cytochrome p450 isoenzymes were studied. Inhibition of 6 isomers of cytochrome p450 in human liver microsomes was studied with the use of specific substrates. It was found that human liver cytochrome p450 enzymes could not induce degradation of GRS and that GRS was not an inductor or inhibitor of cytochrome p450 family members 1A2, 2C9, 2C19, 2D6, 2C8, and 3A4. Hence, clinical use of the prospective antiaggregant would not involve the risk of uncontrolled fluctuations in GRS concentrations in the organism because of interactions between the drugs.

中文翻译:

一种新的抗聚集剂,吲哚酮衍生物的代谢

研究了细胞色素 p450 介导的 GRS(吲哚酮抗聚集剂)代谢及其对细胞色素 p450 同工酶活性的影响。使用特定底物研究了人肝微粒体中细胞色素 p450 的 6 种异构体的抑制作用。发现人肝细胞色素 p450 酶不能诱导 GRS 降解,并且 GRS 不是细胞色素 p450 家族成员 1A2、2C9、2C19、2D6、2C8 和 3A4 的诱导剂或抑制剂。因此,预期抗凝剂的临床使用不会涉及由于药物之间的相互作用而导致生物体内 GRS 浓度不受控制波动的风险。
更新日期:2020-04-01
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