Tetrabenazine: A Reversible Inhibitor of the Vesicular Monoamine Transporter Type 2 (VMAT2)
Tetrabenazine is a reversible selective inhibitor of the vesicular monoamine transporter type 2 (VMAT2) resulting in decreased uptake of monoamines into synaptic vesicles, breaking down of monoamines by monoamine oxidase (MAO) and depletion of monoamine stores. Therefore, tetrabenazine works as a depletor of monoamines (such as dopamine [
A0305], serotonin [
S0370], norepinephrine [
A0906], and histamine [
H0146]) from nerve terminals. Tetrabenazine is metabolitzed by carbonyl reductase to the initial active metabolite dihydrotetrabenazine (HTBZ), a mixture of α-HTBZ and β-HTBZ. HTBZ also inhibits the VMAT2. Although the precise mechanism is unknown, tetrabenazine is effective in treating chorea (Huntington’s disease). In addition, reserpine [
R0007] inhibits VMAT. (The product is for research purpose only.)