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Inhibitors and enhancers of uridine diphosphate-glucuronosyltransferase 2B (UGT2B)

机译:尿苷二磷酸-葡萄糖醛酸转移酶2B(UGT2B)的抑制剂和增强剂

摘要

A UGT2B inhibitor capable of increasing the bio-availability of a drug, is a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: capillarisin, isorhamnetin, β-naphthoflavone, α-naphthoflavone, hesperetin, terpineol, (+)-limonene, β-myrcene, swertiamarin, eriodictyol, cineole, apigenin, baicalin, ursolic acid, isovitexin, lauryl alcohol, puerarin, trans-cinnamaldehyde, 3-phenylpropyl acetate, isoliquritigenin, paeoniflorin, gallic acid, genistein, glycyrrhizin, protocatechuic acid, ethyl myristate, umbelliferone, PEG (Polyethylene glycol) 400, PEG 2000, PEG 4000, Tween 20, Tween 60, Tween 80, BRIJ® 58, BRIJ® 76, Pluronic® F68, Pluronic® F127, and a combination thereof. A UGT2B enhancer capable of enhancing a clearance rate of morphine-like analgesic agents, is a compound in a free base or a pharmaceutically acceptable salt form that is selected from the group consisting of: nordihydroguaiaretic acid, wogonin, trans-cinnamic acid, baicalein, quercetin, daidzein, oleanolic acid, homoorientin, hesperetin, narigin, neohesperidin, (+)-epicatechin, hesperidin, liquiritin, eriodictyol, formononetin, quercitrin, genkwanin, kaempferol, isoquercitrin, (+)-catechin, naringenin, daidzin, (−)-epicatechin, luteolin-7-glucoside, ergosterol, rutin, luteolin, ethyl myristate, apigenin, 3-phenylpropyl acetate, umbelliferone, glycyrrhizin, protocatechuic acid, poncirin, isovitexin, 6-gingerol, cineole, genistein, trans-cinnamaldehyde, and a combination thereof.
机译:能够提高药物的生物利用度的UGT2B抑制剂是游离碱或药学上可接受的盐形式的化合物,选自:毛细血管素,异鼠李素,β-萘黄酮,α-萘黄酮,橙皮素,松油醇,(+)-柠檬烯,β-月桂烯,swertiamarin,eriodictyol,桉树脑,芹菜素,黄in苷,熊果酸,异ovitexin,月桂醇,葛根素,反式肉桂醛,3-苯丙乙酸酯,异异黄体素,pa药苷,没食子酸,genistein甘草酸,原儿茶酸,肉豆蔻酸乙酯,伞形酮,PEG(聚乙二醇)400,PEG 2000,PEG 4000,吐温20,吐温60,吐温80,BRIJ®58,BRIJ®76,Pluronic®F68,Pluronic®F127和它们的组合。一种能够提高吗啡样镇痛药清除率的UGT2B增强剂,是一种游离碱或药学上可接受的盐形式的化合物,选自下组:去甲二氢愈创木酸,wogonin,反式肉桂酸,黄e素,槲皮素,黄豆苷元,齐墩果酸,高Ororientin,橙皮素,萘里汀,新橙皮苷,(+)-表皮儿茶素,橙皮苷,Liquiritin,异黄体醇,甲萘醌,槲皮苷,genkwanin,山胆酚,异槲皮苷,(+)-儿茶酚苷,(+)-儿茶素-表儿茶素,木犀草素7-葡糖苷,麦角固醇,芦丁,木犀草素,肉豆蔻酸乙酯,芹菜素,乙酸3-苯丙酯,伞形酮,甘草甜素,原儿茶酸,poncirin,异ovitexin,6-姜油酚,桉树脑,染料木黄酮,反式肉桂醛和α它们的组合。

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