CAS |
960203-27-4 |
Chinese Name |
氢溴酸沃替西汀 |
English Name |
Vortioxetine Hydrobromide |
Synonyms |
Lu AA21004 hydrobromide |
Molecular Formula |
C18H23BrN2S |
Molecular Weight |
379.36 |
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 |
MFCD00003305 |
SMILES |
CC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C.Br |
InChIKey |
VNGRUFUIHGGOOM-UHFFFAOYSA-N |
InChI |
InChI=1S/C18H22N2S.BrH/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;1H |
PubChem CID |
56843850 |
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 Hydrobromide 是 5-HT1A,5-HT1B,5-HT3A,5-HT7 受体 和5-羟色胺转运体 (SERT) 的抑制剂,其Ki值分别为 15 nM,33 nM,3.7 nM,19 nM 和 1.6 nM。[1] |
In Vitro |
Vortioxetine hydrobromide is a novel multimodal serotonergic 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). [1] |
In Vivo |
In conscious rats,Vortioxetine hydrobromide significantly increased extracellular 5-HT levels in the brain after acute and 3 days of treatment. Following the 3-day treatment(5 or 10(mg/kg)/day)SERT occupancies were only 43% and 57%,respectively. [1]Acute and repeated dosing of vortioxetine(5 or 10(mg/kg)/day)produced more pronounced anxiolytic- and antidepressant-like activities than fluoxetine.[2]Vortioxetine(10mg/day)did not impair driving,cognitive,or psychomotor performance after single or multiple doses.[3]Vortioxetine 5mg did not improve symptoms of generalized anxiety disorder(GAD; HAM-A total score ≥20 and MADRS score ≤16) over 8 weeks of treatment.[4]Vortioxetine has antidepressant- and anxiolytic-like effects in the rat forced swim(Flinders Sensitive Line)and social interaction and conditioned fear tests(minimal effective doses: 7.8,2.0,and 3.9 mg/kg). [5] |
Animal Experiment |
Vortioxetine was assessed in BalB/cJ@RJ mice using the open-field and forced-swim tests(acute: p.o. 1 h,repeated: daily p.o. 21 days),and in 129S6/SvEvTac mice using the novelty suppressed feeding paradigm(acute: p.o. 1 h,sustained: daily p.o. 14 or 21 days). Fluoxetine and diazepam were controls. [2] |
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 |