同义名 :	氯波必利
	CAS号 :	57645-91-7
	货号 :	A666579
	分子式 :	C24H30ClN3O7
	纯度 :	99%+
	分子量 :	507.96
	MDL号 :	MFCD01743960
	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

Clebopride malate, a dopamine antagonist, is therapeutically used for the treatment of peptic ulcer. This drug has potent antidopaminergic activity that causes acute dystonic reaction, parkinsonism and tardive dyskinesia as adverse effects. After cessation of clebopride malate limb dyskinesia disappeared rapidly and respiratory dyskinesia markedly decreased[3]. Clebopride is a class of antidopaminergic gastrointestinal prokinetic. Clebopride at 10 microM significantly decreased the Vmax of phase 0 depolarization and significantly prolonged the action potential duration at 90% repolarization (APD90), whereas the action potential duration at 50% repolarization (APD50) was not prolonged. For hERG (human ether-a-go-go-related gene) potassium channel currents, the IC50 value was 0.62 ± 0.30 microM. Clebopride was found to have no effect on sodium channel currents[4]. Clebopride (0.5, 1.0 and 2.0 mg/kg) promoted significant analgesia in the tail-flick and hot-plate tests and against abdominal constrictions produced by acetic acid or acetylcholine[5]. The adjunct use of Clebopride in PEG (polyethylene glycol electrolyte) solution for colonoscopy preparations tends to increase the acceptability, tolerability, and efficacy. The presence of borborygmus was significantly lower in the Clebopride group[6].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.97mL 0.39mL 0.20mL	9.84mL 1.97mL 0.98mL	19.69mL 3.94mL 1.97mL

参考文献

[1]Bleiberg H, Piccart M, et al. A phase I trial of a new antiemetic drug--clebopride malate--in cisplatin-treated patients. Ann Oncol. 1992 Feb;3(2):141-3. [2]Bleiberg H, Piccart M, et al. A phase I trial of a new antiemetic drug--clebopride malate--in cisplatin-treated patients. Ann Oncol. 1992 Feb;3(2):141-3. [3]Kawasaki H, Yamamoto M, Okayasu H, Wakayama Y. Rinsho Shinkeigaku. 1991;31(8):878‐881 [4]Kim KS, Shin WH, Park SJ, Kim EJ. Effect of clebopride, antidopaminergic gastrointestinal prokinetics, on cardiac repolarization. Int J Toxicol. 2007;26(1):25‐31 [5]Bittencourt SC, De Lima TC, Morato GS. Antinociceptive effects of clebopride in the mouse. Gen Pharmacol. 1995;26(5):1083‐1087 [6]Abdullah M, Rani AA, Fauzi A, et al. A randomized, controlled, double-blind trial of the adjunct use of Clebopride in polyethylene glycol electrolyte (PEG) solution for colonoscopy preparation. Acta Med Indones. 2010;42(1):27‐30