Chlorpromazine

• Description :

  Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

• UNSPSC :

  12352005

• Hazard Statement :

  H301

• Target :

  5-HT Receptor; Autophagy; Cytochrome P450; Dopamine Receptor

• Type :

  Reference compound

• Related Pathways :

  Autophagy; GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling

• Field of Research :

  Cancer; Neurological Disease; Cardiovascular Disease

• Assay Protocol :

  https://www.medchemexpress.com/chlorpromazine.html

• Concentration :

  10mM

• Purity :

  99.75

• Solubility :

  DMSO : 50 mg/mL (ultrasonic)

• Smiles :

  CN(C)CCCN1C2=C(C=CC=C2)SC3=CC=C(Cl)C=C13

• Molecular Formula :

  C17H19ClN2S

• Molecular Weight :

  318.86

• Precautions :

  H301

• References & Citations :

  [1]Kamgar-Dayhoff P, et al. Multifaceted effect of chlorpromazine in cancer: implications for cancer treatment. Oncotarget. 2021 Jul 6;12 (14) :1406-1426. |[2]Shin SY, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells. Carcinogenesis. 2013 Sep;34 (9) :2080-9. |[3]Yang Z, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production. Cell Metab. 2022 Nov 2:S1550-4131 (22) 00461-2. |[4]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. |[5]Thomas D, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol. 2003 Jun;139 (3) :567-74. |[6]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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, protect from light, stored under nitrogen)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  5-HT2 Receptor

• Citation 01 :

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• CAS Number :

  [50-53-3]