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SEP-363856
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SEP-363856图片
CAS NO:1310426-33-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
SEP-856
产品介绍
SEP-363856 (SEP-856) 是具有口服活性的、中枢神经系统活性的抗精神病活性化合物,具有研究精神分裂症的潜力。
生物活性

SEP-363856 (SEP-856), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the study of schizophrenia[1].

IC50& Target[1]

TAAR1

0.140 μM (EC50)

5-HT1AReceptor

2.3 μM (EC50)

5-HT1BReceptor

15.6 μM (EC50)

5-HT1DReceptor

0.262 μM (EC50)

5-HT2AReceptor

>10 μM (EC50)

5-HT2CReceptor

30 μM (EC50)

5-HT7Receptor

6.7 μM (EC50)

体外研究
(In Vitro)

SEP-363856 (10 μM) shows >50% inhibition of specific binding at α2A, α2B, D2, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7receptors[1].

体内研究
(In Vivo)

SEP-363856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs[1].
SEP-363856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity[1].
Oral SEP-363856 administration (1, 3 and 10 mg/kg) produces a dosedependent decrease in REM sleep, increase in latency to REM sleep and increase in cumulative wake (W) time[1].

Animal Model:Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents[1].
Dosage:0.3, 1 and 3 mg/kg.
Administration:Orally once.
Result:Resulted in a dose-dependent inhibition of PCP-induced hyperactivity responses in C57Bl/6J mice (1-way ANOVA F(5, 59)= 18.96, p< 0.0001; Tukey’s post-hoc test, p< 0.05) with a 50% effective dose (ED50) of approximately 0.3 mg/kg.
Animal Model:Male Sprague Dawley rats[1].
Dosage:1, 2, and 5 mg/kg.
Administration:I.V. injection. (Pharmacokinetic Analysis).
Result:0.5 hours in mice and rats and maximum plasma concentrations reached within 6 ± 2.83 hours in monkeys.
Penetrated mouse and rat brains after oral administration (10 mg/kg), with average brain-to-plasma AUC ratios of ~3 respectively.
Clinical Trial
分子量

183.27

Formula

C9H13NOS

CAS 号

1310426-33-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.