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) |
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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].
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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.
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| 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. |
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