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Chlorpromazine HCl

现货
Catalog No.
B1480
多巴胺拮抗剂
组合的产品项目
规格价格库存 数量
1g
¥ 550.00
现货
5g
¥ 900.00
现货
10mM (in 1mL DMSO)
¥ 800.00
现货

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Background

Dopamine receptors are a class of G protein-coupled receptors that are prominent in the central nervous system. Dopamine receptors are implicated in many neurological processes. Thus, dopamine receptors are common neurologic drug targets. Antipsychotics are often dopamine receptor antagonists while typically psychostimulants are indirect agonists of dopamine receptors. Chlorpromazine is a dopamine antagonist.

In vitro: The antipsychotic activity of chlorpromazine has been associated with its ability to act as a dopamine-receptor antagonist. the manner in which chlorpromazine, with its phenothiazine ring structure, interacted with a receptor for dopamine. Furthermore, chlorpromazine inhibited the binding of [3H]spiperone, and the inhibition curve was consistent with a single class of binding sites [1].

In vivo: Daily administration of chlorpromazine to rats for 21 days induced catalepsy, tolerance to catalepsy and locomotor sensitization following PCP challenge. Results suggest that daily chlorpromazine treatment induced DA/NMDA-receptor sensitization to total locomotor activity following PCP challenge [2].

Clinical trial: Chlorpromazine is clinical used as a conventional antipsychotic drug that has been used for the management of psychotic disorders since its FDA approval in 1954.

Reference:
[1] Harrold MW, Chang YA, Wallace RA, Farooqui T, Wallace LJ, Uretsky N, Miller DD.  Charged analogues of chlorpromazine as dopamine antagonists. J Med Chem. 1987 Sep;30(9):1631-5.
[2] Nsimba SE.  Effects of daily chlorpromazine administration on behavioural and physiological parameters in the rat. Indian J Physiol Pharmacol. 2009 Jul-Sep;53(3):209-18.

Chemical Properties

StorageStore at -20°C
M.Wt355.33
Cas No.69-09-0
FormulaC17H19ClN2S.HCl
Solubility≥17.8 mg/mL in DMSO, ≥74.8 mg/mL in EtOH, ≥71.4 mg/mL in H2O
Chemical Name3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride
SDFDownload SDF
Canonical SMILESCN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

海马神经元

制备方法

在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10 ~ 100 μM

实验结果

10 ~ 100 μM的Chlorpromazine HCl呈剂量依赖性地降低mIPSC幅度。此外,当浓度≥ 30 μM时,Chlorpromazine HCl呈剂量依赖性地显著加快mIPSC衰减时间。然而,对照组与Chlorpromazine HCl治疗组的10 ~ 90%上升时间无显著差异。

动物实验 [2]:

动物模型

大鼠缺氧模型

给药剂量

30 mg/kg;腹腔注射

实验结果

在缺氧大鼠模型中,Chlorpromazine HCl减少脑组织突触传递的不可逆缺失。Chlorpromazine HCl还可以减缓Ca2+流入神经元,从而显著延迟缺氧诱导扩散抑制的发生。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Mozrzymas JW, Barberis A, Michalak K, Cherubini E. Chlorpromazine inhibits miniature GABAergic currents by reducing the binding and by increasing the unbinding rate of GABAA receptors. J Neurosci. 1999 Apr 1;19(7):2474-88.

[2]. Balestrino M, Somjen GG. Chlorpromazine protects brain tissue in hypoxia by delaying spreading depression-mediated calcium influx. Brain Res. 1986 Oct 22;385(2):219-26.

质量控制

化学结构

Chlorpromazine HCl