Chlorpromazine (hydrochloride)

Reference compound

Reference compound / Active compounds; API

H301, H330

4°C (Powder, sealed storage, away from moisture and light)

Chlorpromazine hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

DMSO : ≥ 60 mg/mL|H2O : 100 mg/mL (ultrasonic)

Launched

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.
IC50 & Target: Ki: 363 nM (dopamine D₂ receptor), 8.3 nM (5-HT_2A receptor)^[4]
In Vitro: Chlorpromazine (3, 10, 20, 40, and 60 uM) decreases the peak currents of hNav1.7 in a concentration-dependent manner, with IC₅₀ of 25.9 uM with a Hill coefficient of 2.3. Chlorpromazine (25 uM) 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 uM and a Hill coefficient of 1.11. Chlorpromazine (1, 10, 100 uM) 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].

H301, H330