Vesamicol

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Vesamicol
Vesamicol.png
Systematic (IUPAC) name
2-(4-phenyl-1-piperidyl)cyclohexan-1-ol
Clinical data
Legal status ?
Identifiers
CAS number 22232-64-0
ATC code ?
PubChem CID 5662
ChemSpider 5460
ChEMBL CHEMBL20730
Chemical data
Formula C17H25NO 
Mol. mass 259.39 g/mol

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

Mechanism of action[edit]

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 postsynaptic ACh receptor. Vesamicol causes a non-competitive and reversible block of the intracellular transporter VAChT responsible for carrying newly synthesized ACh into secretory vesicles in the presynaptic 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[edit]

  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. doi:10.1007/BF02246498. PMID 8619013.