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.
性状
Solid
IC50 & Target[1][2]
TAAR1 0.140 μM (EC50) 5-HT1A Receptor
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Dedic N, et al. SEP-363856, a Novel Psychotropic Agent with a Unique, Non-D2 Receptor Mechanism of Action. J Pharmacol Exp Ther. 2019 Oct;371(1):1-14.
溶解度数据
In Vitro: H2O : 100 mg/mL (455.10 mM; Need ultrasonic)DMSO : 62.5 mg/mL (284.44 mM; Need ultrasonic)配制储备液