Samelisant 是 H3 受体的特异性反向激动剂，对人和大鼠的 Kis 分别为 8.7 nM 和 9.8 nM。 Samelisant 具有抗猝倒作用，可用于关于发作性睡病的研究。

Samelisant is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

Samelisant (1, 10, and 100 nM) increases the pEC50 from 8.5 to 8.2, 7.3, and 6.2 for human H3 receptor and from 8.2 to 7.9, 7.4, and 6.4 for rat H3 receptor, respectively. Samelisant modulates dopamine and norepinephrine levels in the cerebral cortex. Samelisant reversibly binds to the orthosteric site with Kbs of 1.3 nM and 1.1 nM[1].

In orexin knockout mice subjected to sleep EEG, Samelisant (10 and 30 mg/kg; p.o.) significantly increases wakefulness and concomitantly decreases NREM sleep. Samelisant significantly decreases direct REM sleep onset episodes and dose-dependently increases the level of tele-methylhistamine[1].

1394808-82-2

C21H31N3O3

373.49

SUVN-G3031

DMSO:50 mg/mL (112.01 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years