Ispronicline

Ispronicline is a partial agonist of α4β2 nicotinic acetylcholine receptors (nAChRs).¹ It selectively binds to nAChRs in rat cerebral cortex (K_i = 11 nM) over α7 nAChRs in rat hippocampal membranes (K_i = >50,000 nM).² Ispronicline induces ion flux in thalamic synaptosomes (EC₅₀ = 220 nM) with no effect in T671 muscle cells up to 100 µM, indicating selectivity for α4β2 nAChRs over α3β4 nAChRs.^1,3 It has neuroprotective effects in an in vitro model of oxygen-glucose deprivation using primary rat CA1 hippocampal slices at 100 µM.² Ispronicline (1 mg/animal) enhances recognition memory in mice, an effect that can be blocked by the nAChR antagonist mecamylamine (Item No. 14602).³

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1. Lipiello, P.M., Gatto, G., Bencherif, M., et al. RJR-1734: A potent selective nicotinic ligand that improves cognition acutely and chronically. Soc. Neurosci. Abst. 24 (Part 1), 88 (1998).

2. Gatto, G.J., Bohme, G.A., Caldwell, W.S., et al. TC-1734: An orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects. CNS Drug Rev. 10(2), 147-166 (2004).

3. Obinu, M.C., Reibaud, M., Miquet, J.M., et al. Brain-selective stimulation of nicotinic receptors by TC-1734 enhances ACh transmission from frontoparietal cortex and memory in rodents. Prog. Neuropsychopharmacol. Biol. Psychiatry 26(5), 913-918 (2002).