Target intelligence / Profile preview

Vesicular Monoamine Transporter 2 (VMAT2)

Target
VMAT2
Molecular classification
Transporter, Solute carrier family
01

Overview

VMAT2 is an integral membrane protein responsible for transporting monoamines (dopamine, norepinephrine, serotonin, and histamine) from the cytosol into synaptic vesicles. This packaging is crucial for regulated neurotransmitter release and also plays a role in sequestering toxicants. It operates as a proton-dependent antiporter, utilizing the proton gradient to drive monoamine uptake. Dysregulation of VMAT2 is implicated in neuropsychiatric disorders like Parkinson’s disease and schizophrenia, making it a target for therapeutic drugs and abused substances.

Other names
SLC18A2
02

Mechanism of action

Proton-dependent antiporter; uses the proton gradient generated by vesicular H+-ATPase to drive the uptake of monoamines in exchange for protons.

03

Biological functions

Neurotransmitter transportMonoamine storageSynaptic transmissionToxicant sequestration
04

Disease associations

Parkinson's diseaseSchizophrenia
05

Safety considerations

Broad effects on brain chemistry due to non-selective modulation of multiple monoamines.Potential for drug interactions due to interaction with various compounds including therapeutic and recreational substances.
06

Interacting drugs

Tetrabenazine

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