Mesoridazine benzenesulfonate

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Mesoridazine benzenesulfonate

CAS No. : 32672-69-8

MCE 国际站：Mesoridazine benzenesulfonate

产品活性：Mesoridazine (TPS-23) benzenesulfonate 是硫唑嗪的活性代谢物，是一种具有口服的活性吩噻嗪类抗精神类疾病试剂。Mesoridazine benzenesulfonate 是一种有效、快速的人类醚-a-go-go 相关基因 (hERG) 通道的阻断剂，在 0 mV 时阻断人胚肾 293 细胞 hERG 电流的 IC₅₀ 为 550 nM。Mesoridazine benzenesulfonate 可用于精神分裂症以及某些其他精神疾病的研究。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

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.
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.

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.
Mesoridazine (15 mM) shows intradermal concentration of 0.34 0.74 nmol/mg after topical application on nude mouse back for 6 h.

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