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Samelisant

CAS No. : 1394808-20-8

MCE 国际站：Samelisant

产品活性：Samelisant (SUVN-G3031) 是一种口服有效的，可通过血脑屏障的选择性组胺 H3 受体 (H3R) 反向激动剂。Samelisant 对人类 (hH3R; K_i=8.7 nM) 和大鼠 (rH3R; K_i=9.8 nM) H3R 具有相似的结合亲和力，表明没有种间差异。 Samelisant 可用于研究睡眠相关疾病。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Samelisant displays inverse agonist activity and it exhibits very high selectivity towards H3R. The pEC₅₀ value of histamine (8.5) for human H3 receptor increases to 8.2, 7.3 and 6.2 after treatment with 1, 10 and 100 nM of Samelisant, respectively. The pEC₅₀ value of histamine (8.2) for rat H3 receptor increases to 7.9, 7.4 and 6.4 after treatment with 1, 10 and 100 nmol/L of Samelisant, respectively.
Samelisant binds to the orthosteric site in a reversible manner with K_b values of 1.3 nM and 1.1 nM deduced from pA₂ value for human and rat H3R, respectively.
Samelisant also modulates dopamine and norepinephrine levels in the cerebral cortex while it has no effects on dopamine levels in the striatum or nucleus accumbens.

In Vivo: Treatment with Samelisant (10 and 30 mg/kg, p.o.) produces a significant increase in wakefulness with a concomitant decrease in non-rapid eye movement sleep (NREM) sleep in orexin knockout mice subjected to sleep electroencephalography (EEG).
Samelisant also produces a significant decrease in direct rapid eye movement (REM) sleep onset (DREM) episodes, demonstrating its anticataplectic effects in an animal model relevant to narcolepsy.
Samelisant treatment in mice produces a dose-dependent increase in tele-methylhistamine levels indicating the activation of histaminergic neurotransmission.

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