人肝微粒体和尿苷二磷酸葡萄糖醛酸基转移酶对丁丙诺啡和去甲丁丙诺啡的葡萄糖醛酸化作用。
Glucuronidation of buprenorphine and norbuprenorphine by human liver microsomes and UDP-glucuronosyltransferases.
作者信息
Chang Yan, Moody David E
机构信息
Center for Human Toxicology, Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, UT 84108, USA.
出版信息
Drug Metab Lett. 2009 Apr;3(2):101-7. doi: 10.2174/187231209788654117.
We investigated the enzyme kinetics of buprenorphine and norbuprenorphine glucuronidation in human liver microsomes and UDP-glucuronosyltransferase (UGT) Supersomes. The involvement of UGT 1A1, 1A3 and 2B7 in buprenorpine and 1A3 in norbuprenorphine glucuronidation were confirmed. Novel involvement of 2B17 with buprenorphine and 1A1 with norbuprenorphine were demonstrated. Scaling of buprenorphine clearance with, or without, correction for the nonspecific microsomal protein binding of buprenorphine (f(u) = 0.42) suggested glucuronidation was a significant route for hepatic clearance of buprenorphine.
我们研究了丁丙诺啡和去甲丁丙诺啡在人肝微粒体及UDP-葡萄糖醛酸基转移酶（UGT）超微粒体中的葡萄糖醛酸化酶动力学。证实了UGT 1A1、1A3和2B7参与丁丙诺啡的葡萄糖醛酸化，以及1A3参与去甲丁丙诺啡的葡萄糖醛酸化。证明了2B17与丁丙诺啡、1A1与去甲丁丙诺啡有新的关联。无论是否校正丁丙诺啡非特异性微粒体蛋白结合（f(u)=0.42），丁丙诺啡清除率的标化表明葡萄糖醛酸化是丁丙诺啡肝脏清除的重要途径。
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