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Monoamine TransporterIntroduction There are several different monoamine transporters. DAT, NET and SERT are related to each other and they all consist of a structure of 12 transmembrane helices. Drug action Many drugs, such as antidepressants and psychoactives works on monoamine transporters. Modern antidepressants typically work by enhancing serotonergic or noradrenergic neurotransmission by binding to SERT or NET, and thereby inhibiting reuptake of serotonin and/or norepinephrine and raising active levels in the synapse. Fluoxetine is a selective serotonin reuptake inhibitor and works as a SERT antagonist. Reboxetine is a norepinephrine reuptake inhibitor and works as a NET antagonist. Most psychoactive drugs achieve their effect through interaction with monoamine transporters. The addictive properties of amphetamines and cocaine is thought to come from their ability to inhibit DAT transporter activity.
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