Chlorpromazine hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel and sodium channel. Chlorpromazine binds with D2 and 5HT2A with K_is of 363 nM and 8.3 nM, respectively.

Chlorpromazine (3, 10, 20, 40, and 60 μM) decreases the peak currents of hNav1.7 in a concentration-dependent manner, with IC₅₀ of 25.9 μM with a Hill coefficient of 2.3. Chlorpromazine (25 μM) produces strong use-dependent inhibition of the hNav1.7 current. Chlorpromazine blocks the hNav1.7 channel, independent of calmodulin^[1]. Chlorpromazine blocks HERG potassium channels with an IC₅₀ value of 21.6 μM and a Hill coefficient of 1.11. Chlorpromazine (1, 10, 100 μM) blocks HERG potassium channels expressed in Xenopus laevis oocytes in a concentration-dependent manner. Chlorpromazine blocks HERG potassium channels in the activated state^[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Chlorpromazine (2 mg/kg, i.p.)-induced neurobehavioural abnormalities (NAs) are characterized by significant increase in cataleptic behaviour and loared spontaneous activity reaction time in mice^[2]. Chlorpromazine (1 or 5 mg/kg, i,p.) prevents KET from increasing average spectral power of delta and gamma-high bands on the 5th and 10th days of treatment in rats^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

355.33

C₁₇H₂₀Cl₂N₂S

69-09-0

盐酸氯丙嗪

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vitro: 

DMSO : ≥ 60 mg/mL (168.86 mM)

* “≥” means soluble, but saturation unknown.

*

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (7.04 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (7.04 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.85 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.85 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7

  [2]. Kale OE, et al. An L-type calcium channel blocker, protects against chlorpromazine-induced neurobehavioural deficits in mice. Fundam Clin Pharmacol. 2017 Jan 19

  [3]. Sampaio LR, et al. Electroencephalographic study of chlorpromazine alone or combined with alpha-lipoic acid in a model of schizophrenia in rats. J Psychiatr Res. 2017 Mar;86:73-82

  [4]. Suzuki H, et al. Comparison of the anti-dopamine D2 and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, NSC 170973 and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400

  [5]. Thomas, D., et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol, 2003. 139(3): p. 567-74.

Adult mice (8-10 weeks old) weighing 18-25 g are divided into five groups of six mice per group. The treatment schedule is as follows: Group 1, control (Normal Saline: NS, 10 mL/kg i.p.); Group 2, chlorpromazine (CPZ, 2 mg/kg i.p.); Group 3, CB-154 (BMC, 2.5 mg/kg s.c.); Group 4: AML (1 mg/kg s.c.); Group 5, BMC (2.5 mg/kg s.c.) + AML (1 mg/kg). Animal treated with BMC or AML or their combination also receive chlorpromazine 30 min later (i.p.). Animals are subjected to various tests including metal bar test for catalepsy and spontaneous activity wheel for motor assessment and agility and elevated plus maze, hole-board, Y-maze, open-field tests for locomotory activity, and exploratory behaviour respectively. Animals are euthanized eighteen hours later by cervical dislocation. The brain is dissected, rinsed in buffer (pH 7.6) and homogenized with Teflon and used for assessment of lipid peroxidation, reduced glutathione, superoxide dismutase and catalase.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7

  [2]. Kale OE, et al. An L-type calcium channel blocker, protects against chlorpromazine-induced neurobehavioural deficits in mice. Fundam Clin Pharmacol. 2017 Jan 19

  [3]. Sampaio LR, et al. Electroencephalographic study of chlorpromazine alone or combined with alpha-lipoic acid in a model of schizophrenia in rats. J Psychiatr Res. 2017 Mar;86:73-82

  [4]. Suzuki H, et al. Comparison of the anti-dopamine D2 and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, NSC 170973 and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400

  [5]. Thomas, D., et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol, 2003. 139(3): p. 567-74.