恩他卡朋和托卡朋抑制UGTs引发药物-药物相互作用的研究

来源 :2015第11届全国药物和化学异物代谢学术会议 | 被引量 : 0次 | 上传用户:wodelqm
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  目的 托卡朋和恩他卡朋是新型帕金森病治疗药物。本研究旨在探讨二者对UGTs活性抑制作用,预测UGT1A1抑制引发的潜在药物-药物相互作用(DDI)。方法 以混合人肝微粒体(HLM)及重组表达UGTs作为酶源,选用4-甲基伞形酮(4-MU)、三氟拉嗪(TFP)、N-3-羧丙基-4-羟基-1,8-萘酰亚胺(NCHN)分别为UGTs酶的广谱探针底物,UGT1A4和UGT1A1的特异性探针底物,评估托卡朋和恩他卡朋对12种UGT酶的抑制作用。
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