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Vesamicol

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Vesamicol
Vesamicol.png
Legal status
Legal status
  • Investigational
Identifiers
  • 2-(4-Phenyl-1-piperidyl)cyclohexan-1-ol
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C17H25NO
Molar mass 259.393 g·mol−1
3D model (JSmol)
  • OC1CCCCC1N2CCC(CC2)c3ccccc3

Vesamicol is an experimental drug, acting presynaptically by inhibiting acetylcholine (ACh) uptake into synaptic vesicles and reducing its release. [1] Vesamicol may have applications for the treatment of adenocarcinoma in situ of the lung. [2]

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. [3]

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. doi:10.1007/BF02246498. PMID   8619013. S2CID   25197707.
  2. ↑ Lau JK, Brown KC, Thornhill BA, Crabtree CM, Dom AM, Witte TR, et al. (February 2013). "Inhibition of cholinergic signaling causes apoptosis in human bronchioalveolar carcinoma" (PDF). Cancer Research. 73 (4): 1328–39. doi: 10.1158/0008-5472.CAN-12-3190 . PMC   10461321 . PMID   23222296.
  3. ↑ Zucker RS, Kullmann DM, Kaesar PS (2014). "Release of Neurotransmitters". In Byrne JH, Heidelberger R, Waxham MN (eds.). From Molecules to Networks - An Introduction to Cellular and Molecular Neuroscience\ (3rd ed.). Academic Press. pp. 443–488. doi:10.1016/B978-0-12-397179-1.00015-4. ISBN   978-0-12-397179-1.
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