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Clebopride malate/苹果酸氯波必利 {[allProObj[0].p_purity_real_show]}

货号:A666579 同义名: 氯波必利

Clebopride malate, with antiemetic and prokinetic properties, is a dopamine antagonist drug used to treat gastrointestinal dysfunction.

Clebopride malate/苹果酸氯波必利 化学结构 CAS号:57645-91-7
Clebopride malate/苹果酸氯波必利 化学结构
CAS号:57645-91-7
Clebopride malate/苹果酸氯波必利 3D分子结构
CAS号:57645-91-7
Clebopride malate/苹果酸氯波必利 化学结构 CAS号:57645-91-7
Clebopride malate/苹果酸氯波必利 3D分子结构 CAS号:57645-91-7
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Clebopride malate/苹果酸氯波必利 纯度/质量文件 产品仅供科研

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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

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Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

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Tetrahydroberberine +

D2 receptor, pKi: 6.08

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Prochlorperazine Maleate 98% (HPLC)
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

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Ropinirole HCl ++

D2 receptor, Ki: 29 nM

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Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 99%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

99%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 99%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

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Loxapine succinate ++

D2 receptor (Human), Ki: 62 nM

D1 receptor (human), Ki: 26 nM

++

D2 receptor (bovine), Ki: 26 nM

D2 receptor (human), Ki: 24 nM

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D4 receptor (human), Ki: 7.5 nM

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Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

99%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Clebopride malate/苹果酸氯波必利 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].

Clebopride malate/苹果酸氯波必利 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

Clebopride malate/苹果酸氯波必利 实验方案

计算器
存储液制备 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

Clebopride malate/苹果酸氯波必利 技术信息

CAS号57645-91-7
分子式C24H30ClN3O7
分子量 507.96
SMILES Code O=C(NC1CCN(CC2=CC=CC=C2)CC1)C3=CC(Cl)=C(N)C=C3OC.O=C(O)C(O)CC(O)=O
MDL No. MFCD01743960
别名 氯波必利
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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