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.
体外研究
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-HT7 receptors.
体内研究
SEP-363856 (0.3, 1 and 10 mg/kg, i.p.) is CNS active and exhibits a behavioral signature similar to known antipsychotic drugs.
SEP-363856 (0.3, 1 and 10 mg/kg, orally once) significantly reduces PCP-induced hyperactivity.
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.
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:
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.
分子式
C9H13NOs
分子量
183.27
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.