1. GPCR/G Protein Neuronal Signaling
  2. 5-HT Receptor
  3. (±)-Fabesetron hydrochloride

(±)-Fabesetron hydrochloride  (Synonyms: (±)-FK1052)

目录号: HY-101638
产品使用指南

(±)-Fabesetron hydrochloride ((±)-FK1052) 是 Fabesetron hydrochloride 的消旋体。Fabesetron hydrochloride 是一种有效的 5-HT35-HT4 受体双重拮抗剂。

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(±)-Fabesetron hydrochloride Chemical Structure

(±)-Fabesetron hydrochloride Chemical Structure

CAS No. : 129299-81-6

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Other Forms of (±)-Fabesetron hydrochloride:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

(±)-Fabesetron hydrochloride ((±)-FK1052) is the racemate of Fabesetron hydrochloride, which is a potent 5-HT3 and 5-HT4 receptor dual antagonist[1].

IC50 & Target

5-HT3 Receptor

 

5-HT4 Receptor

 

体内研究
(In Vivo)

In conscious rats, both 5-HT and 5-methoxytryptamine significantly increase fecal pellet output and accelerate colonic transit. In contrast, the effect of 2-methyl-5-HT is slight. Although Ondansetron and Granisetron slightly reduce 5-HT (1 mg/kg s.c.) stimulated colonic transit, (±)-Fabesetron, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit. Furthermore, (±)-Fabesetron, Ondansetron and Granisetron significantly depress the increase in fecal pellet output caused by wrap-restraint stress, with ED50 values of 0.21, 3.0 and 1.1 mg/kg p.o., respectively. Intraperitoneal administration of 5-HT and 5-methoxytryptamine, but not 2-methyl-5-HT, produces a dose-related increase in the incidence of diarrhea in fasted mice. 5-HT (0.32 mg/kg i.p.)-induced diarrhea is also inhibited by (±)-Fabesetron, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively[1]. (±)-Fabesetron (1 mg/kg i.v. ×4) apparently reduces delayed emesis caused by Methotrexate (MTX) and increases, but not significantly, the time for onset of emesis. Furthermore, increasing the dose to 3.2 mg/kg of (±)-Fabesetron also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with (±)-Fabesetron at 1 mg/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

329.82

Formula

C18H20ClN3O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Animal Administration
[1]

Mice and Rats[1]
Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g are used. (±)-Fabesetron, Ondansetron, Granisetron, Methysergide, Ketanserin and Atropine are dissolved in distilled water. 5-HT, 2-methyl-5-HT, 1-phenylbiguanide and 5-MeOT are dissolved in physiological saline. Diazepam is suspended with 0.5% methylcellulose solution. The drugs are administered to rats at a volume of 2 mL/ kg and to mice at a volume of 5 mL/kg.
Dogs[2]
Beagle dogs of either sex weighting 8.0 to18.5 kg are used in the study. Dogs are injected i.v. with MTX (2.5 mg/kg/mL) at 7:30 AM. The animal behavior is recorded using a video camera with an automatic night photographing system for up to 72 h and analyzed at the end of the experiment. (±)-Fabesetron (1 and 3.2 mg/kg), Ondansetron (1 mg/kg), Tropisetron (1 mg/kg), CP-122,721 (0.1 mg/kg), or vehicle (0.5 mL/kg) is administered i.v. at 24, 36, 48, and 60 h after MTX treatment. Episodes of emesis occurring within a few minutes are defined as a single emetic episode. A 12 h artificial light cycle (lights on between 7:30 AM and 7:30 PM) is used throughout the study. Dogs are given a standard laboratory dog chow (300 g/day) and water ad libitum. The animals are retested with MTX at least 6 weeks later.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

(±)-Fabesetron hydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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