Biological Activity
Chlorpromazine Hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel andsodium channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.
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].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.