Ulotaront (SEP-363856, SEP-856)

Chemical Structure : Ulotaront

CAS No.: 1310426-33-5

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货号: PC-72627Not For Human Use, Lab Use Only.

Ulotaront (SEP-363856, SEP-856) is a psychotropic agent and selective agonist of trace amine receptor 1 (TAAR1) and 5-HT1A receptor with EC50 of 0.14 uM and 2.3 uM for human TAAR1 and 5-HT1A receptor respectively, shows no appreciable action at dopamine D2 receptors.

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2480	In stock
25 mg	￥3980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Ulotaront (SEP-363856, SEP-856) is a psychotropic agent and selective agonist of trace amine receptor 1 (TAAR1) and 5-HT1A receptor with EC50 of 0.14 uM and 2.3 uM for human TAAR1 and 5-HT1A receptor respectively, shows no appreciable action at dopamine D2 receptors.

Ulotaront (SEP-363856, SEP-856) exhibits weak partial agonism with EC50 values of 10.44 ± 4 µM (cAMP, Emax = 23.9% ± 7.6%; Fig. 2C) and 8 µM (β-arrestin recruitment, Emax = 27.1%) in D2 receptor functional assays.

Ulotaront (SEP-363856, SEP-856) demonstrates antipsychotic- and antidepressant-like activity without inducing catalepsy.

Ulotaront (SEP-363856, SEP-856) decreases REM sleep in rats.

Ulotaront (SEP-363856, SEP-856) does not exhibit significant occupancy at D2 receptors in nonhuman primates.

Ulotaront (SEP-363856, SEP-856) induces significant inhibitory responses in DPAT-sensitive neurons of the DRN and a subset of VTA neurons.

Ulotaront (SEP-363856, SEP-856) inhibits firing of DRN in vivo and partially attenuates PCP-induced hyperactivity through 5-HT1A receptors.

Ulotaront (SEP-363856, SEP-856) demonstrated broad efficacy in putative rodent models relating to aspects of schizophrenia, including phencyclidine (PCP)-induced hyperactivity, prepulse inhibition, and PCP-induced deficits in social interaction.

物理化学性质&存储条件

分子量	183.269
分子式	C9H13NOS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-[(7S)-5,7-dihydro-4H-thieno[2,3-c]pyran-7-yl]-N-methylmethanamine

参考文献

1. Dedic N, et al. J Pharmacol Exp Ther. 2019 Oct;371(1):1-14.

2. Koblan KS, et al. N Engl J Med. 2020 Apr 16;382(16):1497-1506.