Idalopirdine (Lu AE58054) is a potent, selective 5-HT6 receptor antagonist with Ki of 0.83 nM. Idalopirdine (Lu AE58054) shows no agonist activity in 5-HT(6) GTPgammaS efficacy assay. Idalopirdine (Lu AE58054) demonstrates >50-fold selectivity for >70 targets. Idalopirdine (Lu AE58054) potently inhibits striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157 ([(3)H]8-(4-methylpiperazin-1-yl)-3-phenylsulfonylquinoline), with an ED(50) of 2.7 mg/kg. Idalopirdine (Lu AE58054) exhibits good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia.
