Vesamicol

Vesamicol
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
Formula C17H25NO
Molar mass 259.39 g/mol
3D model (JSmol)

Vesamicol is an experimental drug, acting presynaptically by inhibiting acetylcholine (ACh) uptake into synaptic vesicles and reducing its release.[1] Vesamicol may have applications in BAC therapy.[2] It has been described as a hydroxylated phencyclidine regioisomer.

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 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

  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. doi:10.1007/BF02246498.
  2. ↑ http://cancerres.aacrjournals.org/content/early/2012/12/06/0008-5472.CAN-12-3190.full.pdf
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