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30914-89-7

中文名称 氟甲沙朵
英文名称 Flumexadol
CAS 30914-89-7
分子式 C11H12F3NO
分子量 231.21
MOL 文件 30914-89-7.mol
更新日期 2023/03/20 15:41:21
30914-89-7 结构式 30914-89-7 结构式

基本信息

中文别名
氟甲沙朵
英文别名
1841CERM
CERM-1841
Flumexadol
2-(α,α,α-Trifluoro-m-tolyl)morpholine
2-[3-(Trifluoromethyl)phenyl]morpholine
Morpholine, 2-[3-(trifluoromethyl)phenyl]-

物理化学性质

沸点132 °C(Press: 10 Torr)
密度1.2081 (estimate)
储存条件-20°C储存
溶解度DMSO: 100 mg/mL (432.51 mM)
酸度系数(pKa)8.41±0.40(Predicted)
形态Liquid
颜色Colorless to light yellow

常见问题列表

生物活性
Flumexadol 是一种口服活性非麻醉镇痛药。Flumexadol 是一种选择性和亲和力的 5-HT2C 受体激动剂,对于 Flumexadol 的 (+)-对映体,Ki 为 25 nM,选择性是 5-HT2A 受体的 40 倍。
靶点

5-HT 2C Receptor

25 nM (Ki)

体内研究

In rats and dogs dosed with 14 C-Flumexadol (CERM1841), the 14 C is excreted in the urine. The 14 C eliminated in the faeces of dog is significantly higher than for rat. Conjugated metabolites, mostly glucuronides, accounted for the greater part of the urinary radioactivity in both species. Biotransformation products are predominantly acids in both species, follows by significant amounts of basic metabolites, with very little neutral substances. The major urinary metabolite in rats is 3-trifluoromethylbenzoic acid and 3-trifluoromethylhipuric acid. In the dog it is 3-trifluoromethylmandelic acid in addition to the benzoic acid and its conjugate. The basic products identified in the urine of both species are unchanged drug and 1-amino-2-hydroxy-2-(3-trifluoromethylphenyl)ethane, with the first predominating.

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