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Acetylcholine release inhibitors are compounds that block the release of the neurotransmitter acetylcholine (ACh) from nerve terminals. Primarily exemplified by botulinum neurotoxins, these agents act by cleaving SNARE proteins essential for synaptic vesicle fusion, thereby preventing ACh release into the synaptic cleft. This action leads to reduced cholinergic signaling at neuromuscular junctions, autonomic ganglia, and within the central nervous system, resulting in localized muscle relaxation or reduced glandular activity. Clinical applications include the treatment of muscle spasticity, chronic migraines, overactive bladder, cervical dystonia, excessive sweating (hyperhidrosis), and cosmetic reduction of facial wrinkles.
Blocks presynaptic ACh exocytosis by cleaving SNARE proteins (SNAP25, syntaxin, or synaptobrevin), preventing vesicle fusion and acetylcholine release.
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