產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg 100mg
CAS	960203-27-4
別名
化學名	1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine;hydrobromide
分子式	C18H22N2S.HBr
分子量	379.36
溶解度	≥ 18.968mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Vortioxetine (Lu AA21004) HBr (vortioxetine) is an antidepressant, [1] [2] and a serotonin (5-HT) receptor modulator [1] [3] with Ki values of 3.7 nM, 19 nM, 200 nM, 33 nM, 15 nM, and 1.6 nM, to human (h) 5-HT3A receptor, h5-HT7 receptor, rat (r) 5-HT7 receptor, h5-HT1B receptor, h5-HT1A receptor and h5-HT transporter (hSERT), respectively, with an IC50 value of 2080 nM to r5-HT7 receptor, and with an EC50 value of 460 nM to h5-HT1B receptor [3].

5-HT is important in brain, acting as a neurotransmitter in neuromodulation [4].

In HELA cells expressing h5-HT1B receptors stably, Lu AA21004 displayed a partial agonistic response with an EC50 value of 460±110 nM and an IA of 22%. In a polyclonal HEK-293 cell line expressing the r5-HT7 receptor, Lu AA21004 bound to the r5-HT7 receptor with a Ki value of 200±27 nM and was a functional antagonist at the r5-HT7 receptor with an IC50 value of 2080±18 nM [3].

In rats, subcutaneous (sc) administration of Lu AA21004 resulted in ED50 values of 0.4 mg/kg and 3.2 mg/kg to the rSERT and the r5-HT1B receptor, respectively. Lu AA21004 acted as an antagonist of 5-HT3 receptor with an ED50 value of 0.11 mg/kg sc [3]. Treatment with vortioxetine at doses of 2.5 and 5 mg/kg prior to the acquisition of novel objects made rats show 29 and 33 s, respectively, as average exploration values [5].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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