Definitions

blocking activity

Monoamine transporter

Monoamine transporters are structures in nerve-cell membranes that function as neurotransmitter transporters transferring monoamine neurotransmitters in or out of cells.

Types

There are several different monoamine transporters:

DAT, NET and SERT are related to each other, and each consists of a structure of 12 transmembrane helices.

Drug action

Many drugs, such as antidepressants and psychoactives affect the monoamine transporters.

Modern antidepressants typically work by enhancing serotonergic, noradrenergic or dopaminergic neurotransmission by binding to the corresponding transporter, and thereby inhibiting neurotransmitter reuptake and raising active levels in the synapse. Examples include fluoxetine, a selective serotonin reuptake inhibitor; reboxetine, a norepinephrine reuptake inhibitor and bupropion, which inhibits both the norepinephrine and dopamine transporter.

The euphoric and addictive properties of amphetamine, methamphetamine and cocaine are thought to come from their potent DAT-blocking activity.

See also

References

G.E. Torres, R.R. Gainetdinov and M.G. Caron (2003). "Plasma membrane monoamine transporters: structure, regulation and function". Nat. Rev. Neurosci. 4 (1): 13–25. (Review)

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