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IPSU

CAS No. : 1373765-19-5

MCE 国际站：IPSU

产品活性：IPSU是一种选择性，有口服活性和脑渗透性的OX2R拮抗剂，pK_i值为7.85。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Orexin Receptor (OX Receptor)

In Vitro: Orexin receptor antagonists represent attractive targets for the development of drugs for the treatment of insomnia. IPSU binds rapidly and reaches equilibrium very quickly in binding and/or functional assays.

In Vivo: IPSU has low blood clearance, shows high maximal blood exposure and AUC after oral dosing. It exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration. IPSU increases sleep when dosed during the mouse active phase (lights off); IPSU induces sleep primarily by increasing NREM sleep. IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing. The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day .

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