SEP-363856 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SEP-363856盐酸盐是一种口服活性和中枢神经系统活性精神化合物，具有独特的非D2/5-HT2A作用机制，发挥其抗精神病样作用，具有治疗精神分裂症的潜力。 SEP-856 (10μM) 特异性抑制 α2A、α2B、D2、5-HT1A、5-HT1B、5-HT1D、5-HT2A、5-HT2B、5-HT2C 和 5-HT7 > 50% 受体。

SEP-363856 hydrochloride is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia. SEP-856 (10μM) specifically inhibits α2A, α2B, D2, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C and 5-HT7> 50% receptor.SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active. SEP-856 exhibits a behavioral signature similar to known antipsychotic drugs.PCP-induced hyperactivitysignificantly reduced by SEP-856 (0.3, 1 and 10 mg/kg, orally once) . Oral SEP-856 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.(In Vitro):SEP-856 (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-HT7 receptors.(In Vivo):SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs.SEP-856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity. Oral SEP-856 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.

SEP-856 (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-HT7 receptors.

SEP-856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs.SEP-856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity.?Oral SEP-856 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. Animal Model:Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents.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.Dosage:1, 2, and 5 mg/kg.Administration:I.V. injection. (Pharmacokinetic Analysis).Result:Rapidly absorbed with maximum plasma and brain concentrations reached within 0.25 to 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.

SEP-856 hydrochloride

Endocrinology/Hormones

5-HT Receptor

5-HT1A Receptor|5-HT1B Receptor|5-HT1D Receptor|5-HT2A Receptor|5-HT2C Receptor|5-HT7 Receptor|TAAR1

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1310422-41-3

219.73

C9H14ClNOS

>98% (HPLC)

DMSO:62.5 mg/mL (284.44 mM; Need ultrasonic)

Cl.CNC[C@@H]1OCCc2ccsc12

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(-20℃)

With Ice Pack

≥ 2 years