Inhibitor | Ki | Application | Binding Site Model | ||
---|---|---|---|---|---|
SERT | DAT | NET | |||
nM | |||||
SERT inhibitors | |||||
DASBa | 1 | 1423 | 1350 | PET ligand | |
Sertralineb | 0.1 | 420 | 25 | Therapeutic drug | |
Escitalopramc | 3 | >100,000 | 6514 | Therapeutic drug | Andersen et al., 2010; Koldsø et al., 2010 |
Paroxetined | 0.1 | 490 | 40 | Therapeutic drug | Tavoulari et al., 2009 |
Fluoxetined | 7 | 19,500 | 1020 | Therapeutic drug | Tavoulari et al., 2009 |
Fluvoxamineb | 2 | 1300 | 9200 | Therapeutic drug | |
DAT inhibitors | |||||
GBR12935d | 6800 | 22 | 235 | Pharmacological tool | |
RTI-55e | 4 | 1 | 36 | Pharmacological tool | |
Cocained | 410 | 278 | 910 | Drug of abuse | Beuming et al., 2008 |
CFT WIN 35,428d | 133 | 27 | 33 | Pharmacological tool | Beuming et al., 2008 |
Benztropined | 47,000 | 42 | 292 | Pharmacological tool | |
JHW 007f | 1730 | 25 | 1330 | Pharmacological tool | Beuming et al., 2008 |
NET inhibitors | |||||
Nisoxetined | 400 | 497 | 5 | Pharmacological tool | |
Talopramg | 1400 | 44000 | 3 | Pharmacological tool | |
Talsupramh | 430 | 3900 | 3 | Pharmacological tool | |
Reboxetinei | 242 | >10,000 | 3 | Therapeutic drug | |
Atomoxetinei | 152 | 685 | 5 | Therapeutic drug | |
χ-Conotoxin MrIAj | >100,000 | >100,000 | 1260 | Pharmacological tool | Paczkowski et al., 2007 |
Nomifensineb | 1010 | 56 | 16 | Therapeutic drug | |
Mazindold | 160 | 29 | 3 | Therapeutic drug | |
Amphetaminek,l | 38,460 | 640 | 70 | Drug of abuse | Beuming et al., 2008 |
MDMAl | 2410 | 8290 | 1190 | Drug 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.