| Description |
Chlorpromazine Hydrochloride is an antagonist of the dopamine D2 receptors, 5-HT2A receptors, potassium channel, sodium channel, with Ki of 363 nM and 8.3 nM for dopamine D2 receptor and serotonin 5-HT2A receptor, respectively. |
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| IC50 & Target |
Ki: 363 nM (dopamine D2 receptor), 8.3 nM (5-HT2A receptor)[4] |
| In Vitro |
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]. |
| In Vivo |
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 ketamine (KET) from increasing average spectral power of delta and gamma-high bands on the 5th and 10th days of treatment in rats[3]. |
| Clinical Trial |
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| References |
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| Preparing Stock Solutions |
Please refer to the solubility information to select the appropriate solvent.
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| Animal Administration
[2] |
Chlorpromazine is formulated in saline. 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, bromocriptine (BMC, 2.5 mg/kg s.c.); Group 4: amlodipine (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| References |
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| Molecular Weight |
355.33 |
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| Formula |
C₁₇H₂₀Cl₂N₂S |
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| CAS No. |
69-09-0 |
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| Storage |
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| Shipping | Room temperature in continental US; may vary elsewhere |
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| Solvent & Solubility |
DMSO: ≥ 60 mg/mL
* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> |
Purity: 99.85%
COA (94 KB) HNMR (173 KB) LCMS (205 KB)
Handling Instructions (1252 KB)-
[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. Amlodipine, 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 induced by ketamine 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, haloperidol 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.
