2023年11月1日 · Here we describe cryo-electron microscopy structures of human VMAT2 complexed with serotonin and three clinical drugs at 3.5–2.8 Å, demonstrating the structural basis for transport and inhibition.

VMAT2 inhibitors (vesicular monoamine transporter-2 inhibitors) are used to treat movement disorders such as Huntington’s disease or tardive dyskinesia.

2019年4月2日 · The vesicular monoamine transporter type 2 (VMAT2) inhibitors are agents that cause a depletion of neuroactive peptides such as dopamine in nerve terminals and are used to treat chorea due to neurodegenerative diseases (such as Huntington chorea) or dyskinesias due to neuroleptic medications (tardive dyskinesia).

2023年11月1日 · Here we report cryo-electron microscopy structures of the human vesicular monoamine transporter VMAT2 in complex with the antichorea drug tetrabenazine, the antihypertensive drug reserpine or the...

VMAT2 is the CNS vesicular transporter for not only the biogenic amines DA, NE, EPI, 5-HT, and HIS, but likely also for the trace amines TYR, PEA, and thyronamine (THYR).

In the monoamine system, this process is carried out by the vesicular monoamine transporters (VMAT1 and VMAT2). These proteins are responsible for vesicular packaging of dopamine, norepinephrine, serotonin, and histamine.

2024年1月2日 · Monoamine neurotransmitters such as serotonin and dopamine are loaded by vesicular monoamine transporter 2 (VMAT2) into synaptic vesicles for storage and subsequent release in neurons. Impaired...

Vesicular Monoamine Transporter 2 (VMAT 2) is an integral membrane protein that removes serotonin and other monoamine neurotransmitters from the cytoplasm, packaging them into secretory vesicles for transport and release at the presynaptic terminal. You might find these chapters and articles relevant to this topic.

2025年1月2日 · Vesicular monoamine transporter 2 (VMAT2) is crucial for packaging monoamine neurotransmitters into synaptic vesicles, with their dysregulation linked to schizophrenia, mood disorders, and Parkinson's disease.

2025年3月11日 · VMAT2 inhibitors prevent the transporter from sequestering monoamines into synaptic vesicles, leading to neurotransmitter depletion and reduced release. These inhibitors bind to VMAT2 within presynaptic terminals, disrupting its ability to transport monoamines from the cytoplasm into vesicles.