Mesoridazine

Mesoridazine (TPS-23) , a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine is a potent and rapid open-channel blocker of human ether-a-go-go related gene (hERG) channels and blocks hERG currents with an IC₅₀ of 550 nM (at 0 mV) in human embryonic kidney 293 cells^[1].Mesoridazine can be used for the research of schizophrenia, as well as certain other psychiatric disorders^[1][2]. IC50 & Target:IC₅₀: hERG currents^[1] In Vitro:Mesoridazine blocks human ether-a-go-go-related gene (HERG) currents in a concentration-dependent manner (IC₅₀ = 550 nM at 0 mV), block increased significantly over the voltage range where HERG activates and saturates at voltages eliciting maximal HERG channel activation^[1].
Mesoridazine (15 mM; 24 h) shows total absorption of 15.94 ± 4.04% and 39.24 ± 5.11% in nude mouse and pig skin, respectively^[3]. In Vivo:Mesoridazine (15 mM; topical administration; once or daily for 7 consecutive days) displays potent activity and a long period of analgesia at blocking cutaneous pain^[3].
Mesoridazine (15 mM) shows intradermal concentration of 0.34 0.74 nmol/mg after topical application on nude mouse back for 6 h^[3].