Mesoridazine benzenesulfonate  (Synonyms: TPS-23 benzenesulfonate)

Mesoridazine (TPS-23) benzenesulfonate, a metabolite of Thioridazine (HY-B0965A), acts as an orally active phenothiazine antipsychotic agent. Mesoridazine benzenesulfonate 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 benzenesulfonate can be used for the research of schizophrenia, as well as certain other psychiatric disorders^[1][2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

544.75

C₂₇H₃₂N₂O₄S₃

32672-69-8

O=S(C(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4)C.O=S(C5=CC=CC=C5)(O)=O

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• [1]. Zhi Su, et al. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60.  [Content Brief]

  [2]. I S M Salih, et al. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54.  [Content Brief]

  [3]. Liu KS, et al. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68.  [Content Brief]