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960203-27-4

960203-27-4 structure
960203-27-4 structure
  • Name: Vortioxetine (Lu AA21004) HBr
  • Chemical Name: vortioxetine hydrobromide
  • CAS Number: 960203-27-4
  • Molecular Formula: C18H23BrN2S
  • Molecular Weight: 379.358
  • Catalog: API Nervous system medication Anxiolytic
  • Create Date: 2018-06-22 15:49:05
  • Modify Date: 2024-01-02 12:25:38
  • Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

Name vortioxetine hydrobromide
Synonyms Brintellix
1-{2-[(2,4-Dimethylphenyl)sulfanyl]phenyl}piperazine hydrobromide (1:1)
Piperazine, 1-[2-[(2,4-dimethylphenyl)thio]phenyl]-, hydrobromide (1:1)
UNII:TKS641KOAY
VORTIOXETINE HBr
Vortioxetine hydrobromide
vortioxetine monohydrobromide
1-(2-((2,4-Dimethylphenyl)sulfanyl)phenyl)piperazine monohydrobromide
1-[2-[(2,4-Dimethylphenyl)thio]phenyl]piperazinehydrobromide
1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine hydrobromide
Vortioxetine (hydrobromide)
Description Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
Related Catalog
Target

5-HT1A Receptor:15 nM (Ki)

5-HT1B Receptor:33 nM (Ki)

5-HT3A Receptor:3.7 nM (Ki)

5-HT7 Receptor:19 nM (Ki)

SERT:1.6 nM (Ki)

In Vitro Vortioxetine (Compound 5m) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Vortioxetine displays antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT[1]. Vortioxetine is a partial h5-HT 1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Vortioxetine binds to the r5-HT 7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay[5].
In Vivo Vortioxetine (Lu AA21004) occupies the r5-HT1B receptor and rSERT (ED50= 3.2 and 0.4 mg/kg, respectively) after subcutaneous administration and is a 5-HT3 receptor antagonist[6]. Vortioxetine significantly increases cell proliferation and cell survival and stimulates maturation of immature granule cells in the sub granular zone of the dentate gyrus of the hippocampus after 21 days of treatment[3]. Vortioxetine does not cause cognitive or psychomotor impairment[4].
References

[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 May 28;73C:147-159.

[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, Mahableshwarkar AR, Jacobsen P, Vortioxetine (Lu AA21004) 5mg 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]. Mork 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.

Molecular Formula C18H23BrN2S
Molecular Weight 379.358
Exact Mass 378.076538
PSA 40.57000
LogP 5.21610
Storage condition -20°C

~84%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S; CHRISTENSEN, Kim, Lasse Patent: WO2013/102573 A1, 2013 ; Location in patent: Page/Page column 13; 14 ;

~81%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S Patent: WO2008/113359 A2, 2008 ; Location in patent: Page/Page column 16 ; WO 2008/113359 A2

~%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S Patent: WO2008/113359 A2, 2008 ; Location in patent: Page/Page column 17 ; WO 2008/113359 A2

~83%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S; CHRISTENSEN, Kim, Lasse Patent: WO2013/102573 A1, 2013 ; Location in patent: Page/Page column 14; 15 ;

~%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S Patent: WO2007/144005 A1, 2007 ; Location in patent: Page/Page column 44-45 ; WO 2007/144005 A1

~%

960203-27-4 structure

960203-27-4

Literature: H. LUNDBECK A/S Patent: WO2008/113359 A2, 2008 ; Location in patent: Page/Page column 18 ; WO 2008/113359 A2

~%

960203-27-4 structure

960203-27-4

Literature: Uldam, Henriette Kold; Juhl, Martin; Pedersen, Henrik; Dalgaard, Lars Drug Metabolism and Disposition, 2011 , vol. 39, # 12 p. 2264 - 2274

~%

960203-27-4 structure

960203-27-4

Literature: Uldam, Henriette Kold; Juhl, Martin; Pedersen, Henrik; Dalgaard, Lars Drug Metabolism and Disposition, 2011 , vol. 39, # 12 p. 2264 - 2274

~%

960203-27-4 structure

960203-27-4

Literature: Uldam, Henriette Kold; Juhl, Martin; Pedersen, Henrik; Dalgaard, Lars Drug Metabolism and Disposition, 2011 , vol. 39, # 12 p. 2264 - 2274