| Identification | Back Directory | [Name]
SEP-363856 | [CAS]
1310426-33-5 | [Synonyms]
SEP-856
Ulotaront
SEP-363856
SEP 363856,SEP363856
5H-Thieno[2,3-c]pyran-7-methanamine, 4,7-dihydro-N-methyl-, (7S)- | [Molecular Formula]
C9H13NOS | [MDL Number]
MFCD34470241 | [MOL File]
1310426-33-5.mol | [Molecular Weight]
183.27 |
| Hazard Information | Back Directory | [Uses]
SEP-363856 (SEP-856), an orally active TAAR1 and 5-HT1A agonist 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]. | [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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| [IC 50]
TAAR1: 0.140 μM (EC50); 5-HT1A Receptor: 2.3 μM (EC50); 5-HT1B Receptor: 15.6 μM (EC50); 5-HT1D Receptor: 0.262 μM (EC50); 5-HT2A Receptor: >10 μM (EC50); 5-HT2C Receptor: 30 μM (EC50); 5-HT7 Receptor: 6.7 μM (EC50) | [References]
[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. DOI:10.1124/jpet.119.260281 |
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