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Description: Lu AE58054 hydrochloride (also known as Idalopirdine hydrochloride) is potent and selective antagonist of the 5-HT(6) receptor with Ki value of 0.83 nM. In a 5-HT(6) GTPgammaS efficacy assay, Lu AE58054 showed no agonist activity, but demonstrated potent inhibition of 5-HT-mediated activation. Besides medium affinity to adrenergic alpha(1A)- and alpha(1B)-adrenoreceptors, Lu AE58054 demonstrated > 50-fold selectivity for more than 70 targets examined. Lu AE58054 is in phase III clinical trials as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.
References: Int J Neuropsychopharmacol. 2010 Sep; 13(8):1021-33.
Related CAS#:467459-31-0 (free base)
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