EVP-6124 (hydrochloride)

EVP-6124 is a partial agonist of a7 subunit-containing nicotinic acetylcholine receptors (nAChRs; IC50 = 22.38 nM).{52384} It is 1,000-fold selective for a7 subunit-containing nAChRs over a4B2 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 a7 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).{52385}