Trimethobenzamide HCl

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Chemical Structure| 554-92-7 同义名 : 盐酸曲美苄胺 ;Ro 2-9578; Trimethobenzamide (hydrochloride); Trimethobenzamide hydrochloride
CAS号 : 554-92-7
货号 : A148362
分子式 : C21H29ClN2O5
纯度 : 98%
分子量 : 424.92
MDL号 : MFCD00057999
存储条件:

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Trimethobenzamide HCl is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting. Trimethobenzamide is a (non-phenothiazine) benzamide antiemetic that acts centrally to block D2 receptors, thereby inhibiting the medullary chemoreceptor trigger zone by blocking emetic impulses to the vomiting center[1]. Trimethobenzamide was shown to be significantly better than placebo in relieving periodic and total nausea over the 48-hour study. Vomiting incidence was also reduced in the group receiving trimethobenzamide[2]. Trimethobenzamide HCl was found to have more toxic and teratogenic potential on embryonic growth and development in cultured rat embryos[3]. Open-label studies suggest that the combination of trimethobenzamide and diphenhydramine (TMB/DPH) may provide effective relief in a high proportion of migraineurs[4]. In utero TMB (Trimethobenzamide) exposure may cause growth retardation, neurological damage in the developing brain and intestine, and hepatic damage[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00626327 Meningococcal Infections Phase 3 Completed - -
NCT00626327 - Completed - -
NCT00806195 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.77mL

2.35mL

1.18mL

23.53mL

4.71mL

2.35mL

参考文献

[1]Smith HS, Cox LR, Smith BR. Dopamine receptor antagonists. Ann Palliat Med. 2012;1(2):137‐142

[2]Hurley JD, Eshelman FN. Trimethobenzamide HCl in the treatment of nausea and vomiting associated with antineoplastic chemotherapy. J Clin Pharmacol. 1980;20(5-6 Pt 1):352‐356

[3]Fazliogullari Z, Karabulut AK, Uysal II, Unver Dogan N, Acar H. Investigation of developmental toxicity and teratogenicity of antiemetics on rat Fazliogullari Z, Karabulut AK, Uysal II, Unver Dogan N, Acar H. Investigation of developmental toxicity and teratogenicity of antiemetics on rat embryos cultured in vitro. Anat Histol Embryol. 2013;42(4):239‐246embryos cultured in vitro. Anat Histol Embryol. 2013;42(4):239‐246

[4]Friedman BW, Hochberg M, Esses D, et al. A clinical trial of trimethobenzamide/diphenhydramine versus sumatriptan for acute migraines. Headache. 2006;46(6):934‐941

[5]Goksu Erol AY, Gokcimen A, Ozdemir O. Growth failure, tardive dyskinesia, megacolon development, and hepatic damage in neonatal rats following exposure to trimethobenzamide in utero. J Matern Fetal Neonatal Med. 2011;24(9):1176‐1180