新陈代谢和处置GTS-21,阿尔茨海默氏症的新药物。

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小室Azuma R, M, Korsch BH, Andre JC Onnagawa啊,黑老,马修斯JM

新陈代谢和处置GTS-21,阿尔茨海默氏症的新药物。

Xenobiotica。1999年7月29日(7):747 - 62。

PubMed ID

10456692 (在PubMed

]

文摘

1。GTS-21,新颖的治疗老年痴呆症的药物,是目前临床的发展。在当前的研究中,代谢和处置GTS-21一直在评估老鼠和狗后一次性口服给药和静脉注射的管理。2。口服后[14 c] GTS-21老鼠,放射性物质主要是通过胆汁排泄的粪便(67%)与可能的肝肠循环。尿排泄的放射性物质在老鼠和狗分别是20和19%。3所示。GTS-21口服后迅速而广泛地吸收,从等离子体迅速清除。的最大浓度比率GTS-21总在等离子体辐射低,表明初步的或pre-systemic生物转化。4所示。 In rat, GTS-21 showed linear pharmacokinetics over doses ranging from 1 to 10 mg/kg with an absolute bioavailability of 23%. In dog, the absolute bioavailability was 27% at an oral dose of 3 mg/kg. 5. GTS-21 was O-demethylated to yield compounds that were then subject to glucuronidation. Three of the metabolites in rat urine were isolated and characterized as 4-OH-GTS-21, 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. The major urinary metabolites were 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. 6. In vitro chemical inhibition of cytochrome P450 in human liver microsomes indicated that CYPIA2 and CYP2E1 were the isoforms primarily responsible for the O-demethylation of GTS-21, with some contribution from CYP3A.

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药物

GTS-21

药物酶

药物	酶	类	生物	药理作用	行动
GTS-21	细胞色素P450 1 a2	蛋白质	人类	未知的	底物	细节
GTS-21	细胞色素P450 2 e1	蛋白质	人类	未知的	底物	细节