NS-2359
Chemical compound
Pharmaceutical compound
NS-2359 ATC code
(1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-(methoxymethyl)-8-azabicyclo[3.2.1]octane
PubChem CID UNII Formula C 15 H 19 Cl 2 N O Molar mass −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] phase II clinical trials showed the drug was not effective and not well tolerated.[ 2] [ 1] treatment of ADHD ,[ 3] [ 4] phase I clinical trial exploring the effect of NS-2359 on cocaine -dependent individuals was completed in 2002.[ 5]
See also
References
^ a b "NeuroSearch announces the results of Phase II Proof of Concept studies with NS2359 in depression" . NeuroSearch. Archived from the original on 2016-03-04. Retrieved 2009-06-20 .^ 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 . ^ 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 . ^ Clinical trial number NCT00467428 ClinicalTrials.gov
^ Clinical trial number NCT00032916 ClinicalTrials.gov
DAT Tooltip Dopamine transporter (DRIs Tooltip Dopamine reuptake inhibitors )
NET Tooltip Norepinephrine transporter (NRIs Tooltip Norepinephrine reuptake inhibitors )
Others: Antihistamines (e.g., brompheniramine , chlorphenamine , pheniramine , tripelennamine )Antipsychotics (e.g., loxapine , ziprasidone )Arylcyclohexylamines (e.g., ketamine , phencyclidine )Dopexamine Ephenidine Ginkgo biloba Indeloxazine Nefazodone Opioids (e.g., desmetramadol , methadone , pethidine (meperidine) , tapentadol , tramadol , levorphanol )
SERT Tooltip Serotonin transporter (SRIs Tooltip Serotonin reuptake inhibitors )
Others: A-80426 Amoxapine Antihistamines (e.g., brompheniramine , chlorphenamine , dimenhydrinate , diphenhydramine , mepyramine (pyrilamine) , pheniramine , tripelennamine )Antipsychotics (e.g., loxapine , ziprasidone )Arylcyclohexylamines (e.g., 3-MeO-PCP , esketamine , ketamine , methoxetamine , phencyclidine )Cyclobenzaprine Delucemine Dextromethorphan Dextrorphan Efavirenz Hypidone Medifoxamine Mesembrine Mifepristone MIN-117 (WF-516) N-Me-5-HT Opioids (e.g., dextropropoxyphene , methadone , pethidine (meperidine) , levorphanol , tapentadol , tramadol )Roxindole
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)
