Ulotaront
Based on 11 publication(s) in Google Scholar
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.
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- CAS No.: 1310426-33-5
- Formule: C9H13NOS
- Masse moléculaire:183.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) Ulotaront
More- Nature. 2024 Jun;630(8015):237-246. [Abstract]
- Nature. 2023 Dec;624(7992):672-681. [Abstract]
- Cell. 2023 Nov 22;186(24):5347-5362.e24. [Abstract]
- Adv Sci (Weinh). 2025 Oct 24:e02079. [Abstract]
- J Med Chem. 2025 Apr 10;68(7):7082-7105. [Abstract]
- Front Pharmacol. 2023 Apr 21:14:1161964. [Abstract]
- Drug Dev Res. 2024 Jun;85(4):e22225. [Abstract]
- World J Biol Psychiatry. 2024 Nov 29:1-18. [Abstract]
- Mol Pharmacol. 2025 Jul 28;107(9):100064. [Abstract]
- Synapse. 2025 Mar;79(2):e70011. [Abstract]
- patent. US20260034119A1.
Voir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
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5-HT1A Receptor |
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) |
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute treatment with phencyclidine (PCP), which induces robust hyperactivity in rodents[1].
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Dosage:0.3, 1 and 3 mg/kg.
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Administration:Orally once.
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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.
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Animal Model:Male Sprague Dawley rats[1].
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Dosage:1, 2, and 5 mg/kg.
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Administration:I.V. injection. (Pharmacokinetic Analysis).
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1310426-33-5
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Masse moléculaire 183.27
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Formule C9H13NOS
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SMILES
CNC[C@H]1C2=C(C=CS2)CCO1
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Synonyms
SEP-363856; SEP-856
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (11)
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Journal Impact Factor
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Most Recent
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Nature
2024 Jun;630(8015):237-246. PMID: 38720072 -
Nature
2023 Dec;624(7992):672-681. PMID: 37935376 -
Cell
2023 Nov 22;186(24):5347-5362.e24. PMID: 37963465 -
Adv Sci (Weinh)
Cortico-Striatal-Midbrain Circuit Dysregulation Underlying MK-801 Induced Impulsivity and the Ameliorative Effects of SEP. [Abstract]2025 Oct 24:e02079. PMID: 41133933 -
J Med Chem
Rational Design of the First Dual Agonist at Trace Amine-Associated Receptor 1 and 5-HT2C Receptors Based on Binding Pocket Similarity for the Treatment of Schizophrenia and Alzheimer's Disease-Related Psychosis. [Abstract]2025 Apr 10;68(7):7082-7105. PMID: 40159850 -
Front Pharmacol
Biological evaluation and in silico studies of novel compounds as potent TAAR1 agonists that could be used in schizophrenia treatment. [Abstract]2023 Apr 21:14:1161964. PMID: 37153799 -
Drug Dev Res
SEP-363856 exerts neuroprotection through the PI3K/AKT/GSK-3β signaling pathway in a dual-hit neurodevelopmental model of schizophrenia-like mice. [Abstract]2024 Jun;85(4):e22225. PMID: 38879781 -
World J Biol Psychiatry
SEP-363856 attenuates CUMS-induced depression-like behaviours and reverses hippocampal neuronal injuries. [Abstract]2024 Nov 29:1-18. PMID: 39610275 -
Mol Pharmacol
Trace amine-associated receptor 1 agonists differentially regulate dopamine transporter function. [Abstract]2025 Jul 28;107(9):100064. PMID: 40840012 -
Synapse
Cellular-Resolution and Bulk-Fluorescence Recordings of Calcium Activity Yield Reciprocal Readouts of In Vivo Drug Efficacy. [Abstract]2025 Mar;79(2):e70011. PMID: 40013455 -
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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