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(±)-Vesamicol hydrochloride

CAS: 120447-62-3 F: C17H26ClNO W: 295.85

(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a
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Bioactivity (±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively[1][2].
Target Ki: 2 nM (Vesicular acetylcholine transport), 26 nM (σ1 receptors) and 34 nM (σ2 receptors)
Invitro The pharmacological actions of (±)-Vesamicol have been attributed to inhibition of acetylcholine transport into synaptic vesicles and the subsequent quantal release of acetylcholine[1].
In Vivo (±)-Vesamicol (3 mg/kg; intraperitoneal injection; once; male Wistar rats) treatment increases the levels of cytosolic acetylcholine (ACh) in all regions of the brain, while those of vesicular ACh decreased in all regions except for the striatum[2]. Animal Model:
Name (±)-Vesamicol hydrochloride
CAS 120447-62-3
Formula C17H26ClNO
Molar Mass 295.85
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [1]. S M Efange, et al. N-hydroxyalkyl derivatives of 3 beta-phenyltropane and 1-methylspiro[1H-indoline-3,4'-piperidine]: vesamicol analogues with affinity for monoamine transporters. J Med Chem. 1997 Nov 21;40(24):3905-14. [2]. H Kobayashi, et al. Effects of systemic administration of 2-(4-phenyl-piperidino)-cyclohexanol (vesamicol) and an organophosphate DDVP on the cholinergic system in brain regions of rats. Brain Res Bull. 1997;43(1):17-23.