Vortioxetine (Lu AA21004) HBr

Short Summary : 5-HT receptor modulator, antidepressant and anxiolytic

Category : Neuroscience|5-HT Receptor

Purity : 0.985

CAS Number : 960203-27-4

Formula : C18H22N2S.HBr

Molecular Weight : 379.36

SMILE : CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.Br

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : 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 460110 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 20027 nM and was a functional antagonist at the r5-HT7 receptor with an IC50 value of 208018 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].
References: [1]. 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.[2]. Er-min Gu, Chengke Huang, Bingqing Liang, et al. An UPLCCMS/MS method for the quantitation of vortioxetine in rat plasma: Application to a pharmacokinetic study. J. Chromatogr. B, 2015, 997:70-74.[3]. A. M rk, A. Pehrson, L.T. Brennum, S. M ller 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.[4]. David M. Lovinger. Serotonins Role in Alcohols Effects on the Brain. Alcohol Health & Research World, 1997, 21(2):114-120.[5]. Arne M rk, 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.

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