Chlorpromazine

Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT_2A, 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 hNa_v1.7 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]}. IC50 & Target:D2 dopamine receptors; 5-HT2A^[1][6]. In Vitro:Chlorpromazine (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner^[2].
Chlorpromazine (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later^[2].
Chlorpromazine (20 μM) causes inhibition of cell cycle progression^[2].
Chlorpromazine (10 µM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)^[3].
Chlorpromazine (3, 10, 20, 40, 60 µM) blocks the hNa_v1.7 current in a concentration-dependent manner^[4].
Chlorpromazine blocks HERG potassium channels with an IC₅₀ value of 21.6 µM and a Hill coefficient of 1.11^[5]. In Vivo:Chlorpromazine (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse^[2].