Vesicular Monoamine Transporter 2 - Binding Sites and Ligands

Binding Sites and Ligands

One binding site is that of dihydrotetrabenazine (DTBZ) and reserpine. Lobeline binds at this site. Dextroamphetamine and dextromethamphetamine bind at distinct sites to the VMAT2, inhibiting its function. Although the amphetamines inhibit VMAT2 presynaptically leading to diminished neurotransmitter, the primary mechanism for the enhancement of extracellular monoamines, like dopamine, is reversal of the dopamine transporter (DAT). Other VMAT2 inhibitors such as GZ-793A have been shown to inhibit the reinforcing effects of methamphetamine but without producing stimulant or reinforcing effects themselves.