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NS-2359

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Chemical compound
Pharmaceutical compound
NS-2359
Clinical data
ATC code
  • none
Identifiers
  • (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(methoxymethyl)-8-azabicyclo[3.2.1]octane
PubChem CID
UNII
Chemical and physical data
Formula C15H19Cl2NO
Molar mass 300.22 g·mol−1
3D model (JSmol)
  • Clc1ccc(cc1Cl)C(C2COC)CC3NC2CC3
  • InChI=1S/C15H19Cl2NO/c1-19-8-12-11(7-10-3-5-15(12)18-10)9-2-4-13(16)14(17)6-9/h2,4,6,10-12,15,18H,3,5,7-8H2,1H3/t10-,11+,12+,15+/m0/s1
  • Key:FPTPUYCHSWIWIB-FUTJPDQTSA-N
  (verify)

NS-2359 (GSK-372475) is a serotonin-norepinephrine-dopamine reuptake inhibitor. It was under development by GlaxoSmithKline (GSK) as an antidepressant,[1] but was discontinued in 2009 when phase II clinical trials showed the drug was not effective and not well tolerated.[2] The results did not support further effort by the company.[1] NS-2359 was also in clinical trials for the treatment of ADHD,[3] phase II having been completed in 2007.[4] A phase I clinical trial exploring the effect of NS-2359 on cocaine-dependent individuals was completed in 2002.[5]

See also

[edit ]

References

[edit ]
  1. ^ a b "NeuroSearch announces the results of Phase II Proof of Concept studies with NS2359 in depression". NeuroSearch. Archived from the original on 2016年03月04日. Retrieved 2009年06月20日.
  2. ^ Learned S, Graff O, Roychowdhury S, Moate R, Krishnan KR, Archer G, Modell JG, Alexander R, Zamuner S, Lavergne A, Evoniuk G, Ratti E (May 2012). "Efficacy, safety, and tolerability of a triple reuptake inhibitor GSK372475 in the treatment of patients with major depressive disorder: two randomized, placebo- and active-controlled clinical trials". Journal of Psychopharmacology. 26 (5): 653–62. doi:10.1177/0269881111424931. PMID 22048884. S2CID 9365152.
  3. ^ Wilens TE, Klint T, Adler L, West S, Wesnes K, Graff O, Mikkelsen B (June 2008). "A randomized controlled trial of a novel mixed monoamine reuptake inhibitor in adults with ADHD". Behavioral and Brain Functions. 4: 24. doi:10.1186/1744-9081年4月24日 . PMC 2442604 . PMID 18554401.
  4. ^ Clinical trial number NCT00467428 for "Efficacy and Safety of NS2359 in Adults With Attention Deficit Hyperactivity Disorder" at ClinicalTrials.gov
  5. ^ Clinical trial number NCT00032916 for "Interaction Study With NS2359 and Cocaine in Cocaine Experienced Volunteers" at ClinicalTrials.gov
DAT Tooltip Dopamine transporter
(DRIs Tooltip Dopamine reuptake inhibitors)
NET Tooltip Norepinephrine transporter
(NRIs Tooltip Norepinephrine reuptake inhibitors)
SERT Tooltip Serotonin transporter
(SRIs Tooltip Serotonin reuptake inhibitors)
VMATs Tooltip Vesicular monoamine transporters
Others
2-Carboxymethyl Esters
(3,4-Disubstituted Phenyl)-tropanes
Arylcarboxy
Carboxyalkyl
Acyl
β,α Stereochemistry
α,β Stereochemistry
Heterocycles: 3-Substituted-isoxazol-5-yl
Heterocycles: 3-Substituted-1,2,4-oxadiazole
N-alkyl
N-replaced (S,O,C)
Irreversible
Nortropanes (N-demethylated)
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