药物动力学和代谢[(14)C] -tozadenant (syn - 115),一本小说,负责受体拮抗剂配体,在健康的志愿者。

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Mancel V,数学外汇,面包师P英语年代,克罗夫特,肯尼C,诺特T, Stockis,巴尼M

药物动力学和代谢[(14)C] -tozadenant (syn - 115),一本小说,负责受体拮抗剂配体,在健康的志愿者。

Xenobiotica。2017年8月,47 (8):705 - 718。doi: 10.1080 / 00498254.2016.1221164。Epub 2016 9月2。

PubMed ID

27489076 (在PubMed

]

文摘

1。大酒店这个研究(NCT02240290)旨在探讨人类吸收,性格和质量平衡(14)C-tozadenant,一本小说,负责受体拮抗剂用于帕金森氏症等疾病的临床研究。2。六个健康男性受试者接受单剂量口服tozadenant(240毫克包含81.47 KBq [(14) C] -tozadenant)。血液、尿液和粪便收集超过14天。放射性物质由液体闪烁计数或加速器质谱(AMS)。Tozadenant和代谢物特征使用HPLC-MS /女士和HPLC-AMS分数集合。3所示。在4 h, Cmax tozadenant 1.74杯/毫升,AUC (0-t) 35.0 h杯/毫升,t1/2 15 h, Vz / 1.82 L /公斤,CL / F 1.40毫升/分钟/公斤。((14)C)总辐射,Cmax为2.29杯eq /毫升5 h post-dose和AUC eq (0-t) 43.9 h杯/毫升。 Unchanged tozadenant amounted to 93% of the radiocarbon AUC(0-48h). At 312 h post-dose, cumulative urinary and fecal excretion of radiocarbon reached 30.5% and 55.1% of the dose, respectively. Unchanged tozadenant reached 11% in urine and 12% of the dose in feces. Tozadenant was excreted as metabolites, including di-and mono-hydroxylated metabolites, N/O dealkylated metabolites, hydrated metabolites. 4. The only identified species circulating in plasma was unchanged tozadenant. Tozadenant was primarily excreted in urine and feces in the form of metabolites.

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药物

Tozadenant