A 5-HT6 receptor antagonist
LU AE58054 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 0.83 nM).1 It is selective for 5-HT6 over other 5-HT receptor subtypes (Kis = 250 to >10,000 nM) and 70 other targets but does bind to α1A- and α1B-adrenergic receptors (α1B-ARs; Kis = 21 and 22 nM, respectively). LU AE58054 (5-20 mg/kg) reverses phencyclidine-induced deficits in novel object recognition memory in rats. When administered in combination with the cholinesterase inhibitor rivastigmine , LU AE58054 has an additive effect on the decreased number of slips and falls made by rats with bilateral striatal-dopaminergic and cortical-cholinergic system lesions, a model of Parkinson’s disease motor disruption, in the Michigan complex motor control task.2
1.Arnt, J., Bang-Andersen, B., Grayson, B., et al.Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in ratsInt. J. Neuropsychopharmacol.13(8)1021-1033(2010) 2.Cherian, A.K., Kucinski, A., Wu, R., et al.Co-treatment with rivastigmine and idalopirdine reduces the propensity for falls in a rat model of falls in Parkinson's diseasePsychopharmacology (Berl)236(6)1701-1715(2019)
动态评分
0.0