EVP-6124 (hydrochloride)

EVP-6124 is a partial agonist of α7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC₅₀ = 22.38 nM).¹ It is 1,000-fold selective for α7 subunit-containing nAChRs over α4β2 subunit-containing nAChRs at 10 µM, as well as a panel of 60 peptide and nonpeptide receptors, ion channels, and transporters. EVP-6124 induces inward currents in Xenopus oocytes expressing human α7 subunit-containing nAChRs (EC₅₀ = 0.16 µM). In vivo, EVP-6124 (0.1, 0.3, and 1 mg/kg) reverses scopolamine-induced deficits in the novel object recognition task and prevents natural forgetting of a familiar object in rats. It reduces premature responding, a measure of impulsivity, by low-attentive but not high-attentive female rats in the 5-choice serial reaction time test (5CSRTT).²

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1. Prickaerts, J., van Goethem, N.P., Chesworth, R., et al. EVP-6124, a novel and selective ɑ7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of ɑ7 nicotinic acetylcholine receptors. Neuropharmacology 62(2), 1099-1110 (2012).

2. Hayward, A., Adamson, L., and Neill, J.C. Partial agonism at the α7 nicotinic acetylcholine receptor improves attention, impulsive action and vigilance in low attentive rats. Eur. Neuropsychopharmacol. 27(4), 325-335 (2017).