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Rivanicline is an agonist of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs).1 It selectively induces rubidium ion efflux in M10 cells expressing α4β2 subunit-containing nAChRs (EC50 = 0.73 µM for the chicken channels) over M10 cells expressing α3β4- or α1β1γδ subunit-containing nAChRs (EC50s = >1,000 nM for both for the chicken channels) and a panel of 34 receptors, ion channels, and kinases at 10 µM. It induces contractions in isolated guinea pig ileum (EC30 = 15 µM). Rivanicline (0.6 µmol/kg) prevents scopolamine-induced memory deficits in the passive avoidance test in mice.2 It decreases the number of errors in the radial arm maze in a rat model of ibotenic acid-induced memory impairment when administered at doses of 0.3, 0.6 or 1.2 µmol/kg.
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1. RJR-
2. RJR-