Lu AE 58054 Hydrochloride
Data Sheet
For research use only. Not for human use.
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| CAS No. | 467458-02-2 | Cat. No. | BCP14749 |
| Name | Lu AE 58054 Hydrochloride | ||
| Synonyms | |||
| SMILES | |||
| Chemical Name | |||
| Formula | C20H19F5N2O.HCl | M. Wt | 434.83 |
| Purity | 98% | Storage | Store at 4-8°C |
| Description | IC50 Value: 0.83 nm[1] Target: 5-HT(6)R in vitro: Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki 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. in vivo: Orally administered Lu AE58054 potently inhibited striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157, with an ED(50) of 2.7 mg/kg. Steady-state modelling of an acute pharmacokinetic/5-HT(6)R occupancy time-course experiment indicated a plasma EC(50) value of 20 ng/ml. Administration of Lu AE58054 in a dose range (5-20 mg/kg p.o.) leading to above 65% striatal 5-HT(6)R binding occupancy in vivo, reversed cognitive impairment in a rat novel object recognition task induced after subchronic treatment for 7 d wit | ||
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