AQW-051

AQW-051 is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR).¹ It induces calcium influx in GH3 cells expressing α7 nAChR (EC₅₀ = 38.9 nM). AQW-051 (0.03 or 0.3 mg/kg) improves learning and memory in the social recognition test in mice. It improves learning and memory in the Morris water maze test in rats when administered at a dose of 3 mg/kg. AQW-051 (2, 8, or 15 mg/kg per day) increases the duration of response to L-DOPA-induced increases in coordination in an ovariectomized cynomolgus monkey model of MPTP-induced Parkinson's disease.²

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1. Feuerbach, D., Pezous, N., Weiss, M., et al. AQW051, a novel, potent and selective α7 nicotinic ACh receptor partial agonist: Pharmacological characterization and phase I evaluation. Br. J. Pharmacol. 172(5), (2015).

2. Di Paolo, T., Grégoire, L., Feuerbach, D., et al. AQW051, a novel and selective nicotinic acetylcholine receptor α7 partial agonist, reduces ʟ-Dopa-induced dyskinesias and extends the duration of ʟ-Dopa effects in parkinsonian monkeys. Parkinsonism Relat. Disord. 20(11), 1119-1123 (2014).