Vortioxetine (Lu AA21004) HBr
Vortioxetine (Lu AA21004) HBr (vortioxetine) is an antidepressant,   and a serotonin (5-HT) receptor modulator   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 .
5-HT is important in brain, acting as a neurotransmitter in neuromodulation .
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 .
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 . 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 .
. Connie Sanchez, Karen E. Asin, Francesc Artigas, et al. Vortioxetine, a novel antidepressant with multimodal activity: Review of preclinical and clinical data. Pharmacology & Therapeutics, 2015, 145:43-57.
. Er-min Gu, Chengke Huang, Bingqing Liang, et al. An UPLC–MS/MS method for the quantitation of vortioxetine in rat plasma: Application to a pharmacokinetic study. J. Chromatogr. B, 2015, 997:70-74.
. A. Mørk, A. Pehrson, L.T. Brennum, S. Møller Nielsen, et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J. Pharmacol. Exp. Ther., 2012, 340:666-675.
. David M. Lovinger. Serotonin’s Role in Alcohol’s Effects on the Brain. Alcohol Health & Research World, 1997, 21(2):114-120.
. Arne Mørk, Liliana P. Montezinho, Silke Miller, et al. Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacology, Biochemistry and Behavior, 2013, 105:41-50.
|Storage||Store at -20°C|
|Solubility||≥18.968mg/mL in DMSO|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|