TABLE 3

Inhibitors of monoamine transporters

InhibitorKiApplicationBinding Site Model
SERTDATNET
nM
SERT inhibitors
    DASBa114231350PET ligand
    Sertralineb0.142025Therapeutic drug
    Escitalopramc3>100,0006514Therapeutic drugAndersen et al., 2010; Koldsø et al., 2010
    Paroxetined0.149040Therapeutic drugTavoulari et al., 2009
    Fluoxetined719,5001020Therapeutic drugTavoulari et al., 2009
    Fluvoxamineb213009200Therapeutic drug
DAT inhibitors
    GBR12935d680022235Pharmacological tool
    RTI-55e4136Pharmacological tool
    Cocained410278910Drug of abuseBeuming et al., 2008
    CFT WIN 35,428d1332733Pharmacological toolBeuming et al., 2008
    Benztropined47,00042292Pharmacological tool
    JHW 007f1730251330Pharmacological toolBeuming et al., 2008
NET inhibitors
    Nisoxetined4004975Pharmacological tool
    Talopramg1400440003Pharmacological tool
    Talsupramh43039003Pharmacological tool
    Reboxetinei242>10,0003Therapeutic drug
    Atomoxetinei1526855Therapeutic drug
    χ-Conotoxin MrIAj>100,000>100,0001260Pharmacological toolPaczkowski et al., 2007
    Nomifensineb10105616Therapeutic drug
    Mazindold160293Therapeutic drug
    Amphetaminek,l38,46064070Drug of abuseBeuming et al., 2008
    MDMAl241082901190Drug of abuse
  • DASB, 3-amino-4-(2-dimethylaminomethyl-phenylsulfanyl)benzonitrile; GBR12935, 1-(2(diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine; WIN 35,428, 2β-carbomethoxy-3β-(4-fluorophenyl)tropane.

  • a Wilson et al., 2000.

  • b Tatsumi et al., 1997.

  • c Owens et al., 2001.

  • d Eshleman et al., 1999.

  • e Carroll et al., 1995.

  • f Agoston et al., 1997.

  • g Bøgesø et al., 1985.

  • h McConathy et al., 2004.

  • i Andersen et al., 2009a.

  • j Sharpe et al., 2001.

  • k Synthetic substrates.

  • l Han and Gu, 2006.