降脂的性质tak - 475,角鲨烯合酶抑制剂,体内和体外。

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Nishimoto T,天野之弥Y, Tozawa R,石川E, Imura Y, Yukimasa H, Sugiyama Y

降脂的性质tak - 475,角鲨烯合酶抑制剂,体内和体外。

Br J杂志。2003年7月,139 (5):911 - 8。

PubMed ID

12839864 (在PubMed

]

文摘

1。角鲨烯合成酶的酶转换通过焦磷酸中角鲨烯胆固醇生物合成途径。我们检查了降脂的性质1 - [[(3 r, 5 s) 1 - (3-acetoxy-2, 2-dimethylpropyl) 7-chloro-5 - (2, 3-dimethoxyphenyl) 2 o xo-1, 2, 3, 5-tetrahydro-4, 1-benzoxazepin-3-yl]乙酰]piperidine-4-acetic酸(tak - 475),一本小说角鲨烯合酶抑制剂。2。tak - 475抑制肝脏胆固醇生物合成的老鼠(ED(50), 2.9毫克公斤(1))和显示降脂效果的小猎犬狗,狨猴,猕猴和纯种肥老鼠。3所示。在狨猴,tak - 475(100毫克公斤(1)订单。4天)降低等离子体非高密度脂蛋白(HDL)胆固醇和甘油三酸酯,但不影响血浆高密度脂蛋白胆固醇。另一方面,阿托伐他汀(10、30毫克公斤(1)订单。4天)降低了所有这些脂质水平。之间的相关性降低甘油三酯和高密度脂蛋白胆固醇增加,tak - 475增加高密度脂蛋白胆固醇和甘油三酯下降低于阿托伐他汀。 4. TAK-475 (60 mg kg(-1), p.o., for 15 days) suppressed the rate of triglyceride secretion from the liver in hypertriglyceridemic Wistar fatty rats, which show an enhanced triglyceride secretion rate from the liver compared with their lean littermates. 5. In HepG2 cells, TAK-475 and its pharmacologically active metabolite, T-91485, increased the binding of (125)I-low-density lipoprotein (LDL) to LDL receptors. 6. These results suggest that TAK-475 has clear hypolipidemic effects in animals via inhibition of hepatic triglyceride secretion and upregulation of LDL receptors, and that TAK-475 might increase HDL cholesterol by decreasing triglyceride. Thus, TAK-475 is expected to be useful for the treatment of dyslipidemia.

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药物

tak - 475