Vesamicol
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| Identifiers | |
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| CAS Number | 22232-64-0 |
| PubChem (CID) | 5662 |
| IUPHAR/BPS | 4759 |
| ChemSpider | 5460 |
| ChEMBL | CHEMBL20730 |
| Chemical and physical data | |
| Formula | C17H25NO |
| Molar mass | 259.39 g/mol |
| 3D model (Jmol) | Interactive image |
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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[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]
- ^ 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.
- ^ http://cancerres.aacrjournals.org/content/early/2012/12/06/0008-5472.CAN-12-3190.full.pdf
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