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编 号:F624815
分子式:C9H14ClNOS
分子量:219.73
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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生物活性:
SEP-363856 hydrochloride (SEP-856 hydrochloride), 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 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia.

体内研究:
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.

体外研究:
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.
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