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Vesamicol
Systematic (IUPAC) name
2-(4-phenyl-1-piperidyl)cyclohexan-1-ol
Identifiers
CAS number 22232-64-0
ATC code  ?
PubChem 5662
ChemSpider 5460
Chemical data
Formula C17H25NO
Mol. mass 259.39 g/mol
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

Vesamicol is an experimental drug, acting presynaptically by inhibiting acetylcholine (ACh) uptake and reducing its release.[1]

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. Blocking of acetylcholine loading leads to empty vesicles fusing with neuron membranes, decreasing Ach release.

References

  1. ^ Salin-Pascual RJ, Jimenez-Anguiano A (October 1995). "Vesamicol, an acetylcholine uptake blocker in presynaptic vesicles, suppresses rapid eye movement (REM) sleep in the rat". Psychopharmacology 121 (4): 485–7. PMID 8619013. 
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