主要参与兔肝细胞色素P4501A噻苯咪唑5-hydroxylation。

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Rey-Grobellet X, Eeckhoutte C,经摩根富林明,Alvinerie M, Galtier P

主要参与兔肝细胞色素P4501A噻苯咪唑5-hydroxylation。

Xenobiotica。1996年7月,26 (7):765 - 78。

PubMed ID

8819304 (在PubMed

]

文摘

1。噻苯咪唑是一种广泛使用的食品防腐剂和驱虫剂药物饲养动物。为了精确描述细胞色素P450同工酶(s)参与代谢的主要途径,快速和敏感spectrofluorimetric方法开发的同时测定肝噻苯咪唑及其主要代谢物5-hydroxythiabendazole。2。噻苯咪唑的动力学5-hydroxylation测定微粒体准备从控制兔子或动物以前对待beta-naphthoflavone异黄樟素、苯巴比妥、利福平或安妥明。这些疗法导致特定的CYP1A1感应,1 a2, 2 b4, 3 a6和4分别a1。3所示。通过考虑这个面板的特征微粒体准备,只有那些从BNF-treated兔子展出获得增加噻苯咪唑5-hydroxylase活动Ethoxyresorufin O-deethylation在这些微粒体由噻苯咪唑完全抑制。这些主张的具体参与CYP1A亚科。4所示。 In the CYP1A subfamily, CYP1A2 appears to be responsible for basal 5-hydroxylation and further unidentified metabolism of thiabendazole in control livers. However, the major involvement of CYP1A1 is supported by the following characteristics of 5-hydroxylation of thiabendazole: (1) the correlation with CYP1A1 expression and (2) the inhibition by ellipticine and not by furafylline, inhibitors of CYP1A1 and CYP1A2 respectively. 5. All these data demonstrated that the rabbit cytochrome P4501A is predominantly involved in thiabendazole 5-hydroxylation which has been suspected to be critical in terms of safety of the parent drug.

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药物酶

药物	酶	类	生物	药理作用	行动
安妥明	细胞色素P450 1 a1	蛋白质	人类	未知的	诱导物	细节