Monoamine Transporter - Psychostimulants

Psychostimulants

DAT is also the target of several “DAT-blockers” including amphetamines and cocaine. These chemicals inhibit the action of DAT and, to a lesser extent, the other monoamine transporters, but their effects are mediated by separate mechanisms.

Monoamine transporters are established targets for many pharmacological agents that affect brain function, including the psychostimulants cocaine and amphetamines. Cocaine and amphetamines employ different mechanisms that both result in an increase in extracellular monoamines by decreasing reuptake. Psychostimulants affect primarily DAT, although there is some inhibition at SERT and NET. Large increases in synaptic dopamine result in increased stimulation of target neurons believed to create the sensations of cocaine and amphetamines.