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. Author manuscript; available in PMC: 2018 Dec 20.
Published in final edited form as: Curr Protoc Pharmacol. 2017 Dec 20;79:12.16.1–12.16.17. doi: 10.1002/cpph.32

Table 1.

Commonly known ligands of monoamine transporters.

Transporters DAT NET SERT
Endogenous Substrates dopamine (DA) norepinephrine (NE), dopamine (DA) 5-hydroxytryptamine (5-HT, serotonin)
Synthetic substrates amphetamine, methamphetamine, 1-methyl-4-phenylpyridinium (MPP+) amphetamine, methamphetamine, 1-methyl-4-phenylpyridinium (MPP+) MDMA, 1-methyl-4-phenylpyridinium (MPP+)
Releasers or efflux promoters amphetamine, MDMA, phenmetrazine amphetamine, MDMA, phenmetrazine amphetamine, MDMA, 1-(3-trifluoromethylphenyl) Piperazine (TPP)
Inhibitors Compound Function Compound Function Compound Function
Cocaine Drug of abuse Nisoxetine Pharmacological tool Paroxetine Therapeutic drug
Bupropion Therapeutic drug Talopram Pharmacological tool Sertraline Therapeutic drug
GBR12935 Pharmacological tool Reboxetine Therapeutic drug citalopram Therapeutic drug
Methylphenidate Therapeutic drug Nomifensin Therapeutic drug Fluoxetine Therapeutic drug
WIN35428 Pharmacological tool Mazindol Therapeutic drug Fluvoxamine Therapeutic drug
RTI-55 Pharmacological tool Amphetamine Drug of abuse amitriptyline Therapeutic drug
nomifensin Therapeutic drug MDMA Drug of abuse desipramine Therapeutic drug
benztropine Pharmacological tool methylphenidate Therapeutic drug trimipramine Therapeutic drug
JHW 007 Pharmacological tool Clomipramine Therapeutic drug Clomipramine Therapeutic drug
Commonly used radiolabelled inhibitors [3H]-GBR12935, [3H]-WIN35428, [3H]-RTI-55 [3H]-mazindol, [3H]-nisoxetine, [3H]-RTI-55 [3H]-paroxetine, [3H]-citalopram, [3H]-RTI-55