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30914-89-7

中文名稱 氟甲沙朵
英文名稱 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 結(jié)構(gòu)式 30914-89-7 結(jié)構(gòu)式

基本信息

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

物理化學性質(zhì)

沸點132 °C(Press: 10 Torr)
密度1.2081 (estimate)
儲存條件-20°C儲存
溶解度DMSO: 100 mg/mL (432.51 mM)
酸度系數(shù)(pKa)8.41±0.40(Predicted)
形態(tài)Liquid
顏色Colorless to light yellow

常見問題列表

生物活性
Flumexadol 是一種口服活性非麻醉鎮(zhèn)痛藥。Flumexadol 是一種選擇性和親和力的 5-HT2C 受體激動劑,對于 Flumexadol 的 (+)-對映體,Ki 為 25 nM,選擇性是 5-HT2A 受體的 40 倍。
靶點

5-HT 2C Receptor

25 nM (Ki)

體內(nèi)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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