Vesamicol
Vesamicol
Chemical compound
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]
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Formula | C17H25NO |
Molar mass | 259.393 g·mol−1 |
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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]
- 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.
- 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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