Biological Activity
IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
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[2].
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 [1].
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.
