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NS-2359

From Wikipedia, the free encyclopedia
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
PubChemCID
UNII
Chemical and physical data
FormulaC15H19Cl2NO
Molar mass300.22 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 aserotonin-norepinephrine-dopamine reuptake inhibitor. It was underdevelopment byGlaxoSmithKline (GSK) as anantidepressant,[1] but was discontinued in 2009 whenphase IIclinical 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 thetreatment ofADHD,[3] phase II having been completed in 2007.[4] Aphase I clinical trial exploring the effect of NS-2359 oncocaine-dependent individuals was completed in 2002.[5]

See also

[edit]

References

[edit]
  1. ^ab"NeuroSearch announces the results of Phase II Proof of Concept studies with NS2359 in depression". NeuroSearch.Archived from the original on 2016-03-04. Retrieved2009-06-20.
  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:10.1186/1744-9081-4-24.PMC 2442604.PMID 18554401.
  4. ^Clinical trial numberNCT00467428 for "Efficacy and Safety of NS2359 in Adults With Attention Deficit Hyperactivity Disorder" atClinicalTrials.gov
  5. ^Clinical trial numberNCT00032916 for "Interaction Study With NS2359 and Cocaine in Cocaine Experienced Volunteers" atClinicalTrials.gov
DATTooltip Dopamine transporter
(DRIsTooltip Dopamine reuptake inhibitors)
NETTooltip Norepinephrine transporter
(NRIsTooltip Norepinephrine reuptake inhibitors)
SERTTooltip Serotonin transporter
(SRIsTooltip Serotonin reuptake inhibitors)
VMATsTooltip 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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