Physiological antagonist


Vesamicol is an experimental drug, acting presynaptically on acetylcholine (ACh) synthesis.

Mechanism of action

Vesamicol can be broadly categorized as a cholinergic physiological antagonist, because it reduces the apparent activity of cholinergic neurons, but does not act at the post-synaptic ACh receptor. Vesamicol causes a non-competitive and reversible block of the intracellular transporter responsible for carrying newly synthesised ACh into storage vesicles in the pre-synaptic nerve terminal. This transport process is driven by a proton gradient between cell organelles and the cytoplasm.


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