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Flumexadol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Flumexadol图片
CAS NO:30914-89-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.30914-89-7
别名氟甲沙朵
Canonical SMILESFC(C1=CC(C2CNCCO2)=CC=C1)(F)F
分子式C11H12F3NO
分子量231.21
溶解度DMSO: 100 mg/mL (432.51 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Flumexadol is an orally active non-narcotic analgesic. Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor[1][2].

In rats and dogs dosed with 14C-Flumexadol (CERM1841), the 14C is excreted in the urine. The 14C 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[3].

[1]. Hache J, et al. The pharmacology of 1841 CERM, a new analgesic. Arzneimittelforschung. 1978;28(4):642-5. [2]. Nilsson BM. 5-Hydroxytryptamine 2C (5-HT2C) receptor agonists as potential antiobesity agents. J Med Chem. 2006 Jul 13;49(14):4023-34. [3]. Kucharczyk N, et al. Metabolites of 2-(3-trifluoromethylphenyl)tetrahydro-1,4-oxazine (CERM) 1841) in rats and dogs. Xenobiotica. 1979 Nov;9(11):703-11.