| CAS |
508233-74-7 |
| Chinese Name |
沃替西汀 |
| English Name |
Vortioxetine |
| Synonyms |
Lu AA 21004 |
| Molecular Formula |
C18H22N2S |
| Molecular Weight |
298.45 |
| Solubility |
Soluble in DMSO(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
Light yellow to yellow Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00867591 |
| SMILES |
CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C |
| InChIKey |
YQNWZWMKLDQSAC-UHFFFAOYSA-N |
| InChI |
InChI=1S/C18H22N2S/c1-14-7-8-17(15(2)13-14)21-18-6-4-3-5-16(18)20-11-9-19-10-12-20/h3-8，13，19H，9-12H2，1-2H3 |
| PubChem CID |
9966051 |
| Target Point |
5-HT Receptor;Serotonin Transporter |
| Passage |
Neuronal Signaling；GPCR & G Protein |
| Background |
It is an inhibitor of the 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and the serotonin transporter (SERT). |
| Biological Activity |
Vortioxetine 是 5-HT1A、5-HT1B、5-HT3A、5-HT7 受体和 SERT 的抑制剂，其 Ki 值分别为 15 nM、33 nM、3.7 nM、19 nM 和 1.6 nM。Vortioxetine具有抗抑郁作用。[5] |
| In Vitro |
Vortioxetine was the lead compound，displaying high affinity for recombinant human 5-HT(1A)(K(i)= 15 nM)，5-HT(1B)(K(i)= 33 nM)，5-HT(3A)(K(i)= 3.7 nM)，5-HT(7)(K(i)= 19 nM)，and noradrenergic β(1)(K(i)= 46 nM)receptors，and SERT(K(i)= 1.6 nM). Vortioxetine displayed antagonistic properties at 5-HT(3A)and 5-HT(7)receptors，partial agonist properties at 5-HT(1B)receptors，agonistic properties at 5-HT(1A)receptors，and potent inhibition of SERT.[1] Vortioxetine is a partial h5-HT(1B)receptor agonist [EC(50)= 460 nM. Vortioxetine is a rat(r)5-HT(7)receptor antagonist(K(i)= 200 nM and IC(50)= 2080 nM). Vortioxetine occupies the r5-HT(1B)receptor and rSERT(ED(50)= 3.2 and 0.4 mg/kg)and a 5-HT(3)receptor antagonist(ED(50)= 0.11 mg/kg s.c.).[5] |
| In Vivo |
Vortioxetine(5 or 10(mg/kg)/day，rats，3 days)significantly increased extracellular 5-HT levels in the brain after acute and 3 days of treatment.[1] Vortioxetine(acute: p.o. 1 h，sustained: daily p.o. 14 or 21 days)displays an antidepressant and anxiolytic profile following repeated administration associated with increased neurogenesis at several stages.[2] Vortioxetine(10 mg，15 days)did not impair driving，cognitive，or psychomotor performance after single or multiple doses.[3] Vortioxetine(5mg，8 weeks)did not improve symptoms of GAD over 8 weeks of treatment，and was well tolerated.[4] Vortioxetine(5 mg/kg per day for 3 days; minipump subcutaneously)，significantly increased extracellular 5-HT in the ventral hippocampus. Vortioxetine has antidepressant- and anxiolytic-like effects in the rat(minimal effective doses: 7.8，2.0，and 3.9 mg/kg).[5] |
| Data Literature Source |
[1]. Bang-Andersen B，et al. Discovery of 1-[2-(2，4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011 May 12;54(9):3206-21.
[2]. Guilloux JP，et al. Antidepressant and anxiolytic potential of the multimodal antidepressant vortioxetine (Lu AA21004) assessed by behavioural and neurogenesis outcomes in mice. Neuropharmacology. 2013 Oct;73:147-59.
[3]. Theunissen EL，et al. A randomized trial on the acute and steady-state effects of a new antidepressant，vortioxetine (Lu AA21004)，on actual driving and cognition. Clin Pharmacol Ther. 2013 Jun;93(6):493-501.
[4]. Rothschild AJ，et al. Vortioxetine (Lu AA21004) 5 mg in generalized anxiety disorder: results of an 8-week randomized，double-blind，placebo-controlled clinical trial in the United States. Eur Neuropsychopharmacol. 2012 Dec;22(12):858-66.
[5]. M rk A，et al. Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder. J Pharmacol Exp Ther. 2012 Mar;340(3):666-75. |
| Unit |
Bottle |
| Specification |
10mg 50mg |
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