产品
编 号：F149541
分子式：C21H33Cl2N3O3
分子量：446.41
分子式：C21H33Cl2N3O3
分子量：446.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1394808-20-8
产品详情
生物活性：
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
体内研究：
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.Animal Model:Male Wistar rats or male C57BL6J mice
Dosage:1, 3, 10, and 30 mg/kg
Administration:Oral administration
Result:Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats.Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.
体外研究：
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 Kb 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.
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders.
体内研究：
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.Animal Model:Male Wistar rats or male C57BL6J mice
Dosage:1, 3, 10, and 30 mg/kg
Administration:Oral administration
Result:Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats.Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.
体外研究：
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 Kb 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.
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