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VMAT2 substrate (vesicular release)

• Transported INTO the vesicle, alkalinizing it and driving reverse transport
• ➔ monoamine floods the cytoplasm and exits through DAT/NET
• ⚑ Opposite outcome to VMAT2 inhibition: massive synaptic release, not depletion
• Underlies the euphoria and neurotoxicity of amphetamine-type stimulants

Drugs with this mechanism (1)

• Methamphetamine — Potent, CNS-penetrant amphetamine; high addiction liability, rare medical use.

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