(±)-Vesamicol (hydrochloride)

(±)-Vesamicol is an acetylcholine (ACh) uptake inhibitor (IC50 = 40 nM) and neuromuscular blocking agent. It binds to the vesamicol receptor (Ki = 2 nM), as well as sigma non-opioid intracellular receptor 1 (sigma1-receptor) and sigma intracellular receptor 2 (sigma2-receptor, Kis = 26 and 34 nM, respectively). (±)-Vesamicol (150 µg/kg) inhibits electrically induced maximal twitches of tibialis anterior muscles in anesthetized cats. It induces transient flaccid paralysis in conscious mice when administered intravenously or orally (ED50s = 2. and 35. mg/kg, respectively). Intracerebroventricular administration of (±)-vesamicol (80 or 100 µg/animal) decreases rapid eye movement (REM) sleep frequency and duration in rats.. Solulibility: DMSO: Slightly soluble: 0.1-1 mg/ml: Ethanol: Sparingly soluble: 1-10 mg/ml, PBS (pH 7.2): Sparingly soluble: 1-10 mg/ml.