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Lu AE58054 hydrochloride
- Idalopirdine HCl
- Parent CAS: 467459-31-0
- Soluble in water and DMSO
- MF: C20H19F5N2O.HCl
- MW: 434.83
Description
5-HT6 receptor antagonist (Ki value 0.83 nM for h5-HT6) demonstrating >50-fold selectivity for more than 70 targets examined, with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Idalopirdine (Lu AE58054) potentiates the effects of Donepezil (Axon 1438) on two pharmacodynamic biomarkers associated with cognition, i.e. neuronal oscillations and extracellular ACh levels in the hippocampus.
More Information
| Parent CAS No. | 467459-31-0 |
|---|---|
| Chemical Name | 2-(6-fluoro-1H-indol-3-yl)-N-(3-(2,2,3,3-tetrafluoropropoxy)benzyl)ethanamine hydrochloride |
| SMILES | N1C2=C(C=CC(F)=C2)C(CCNCC2=CC=CC(OCC(F)(F)C(F)F)=C2)=C1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C20H19F5N2O.ClH/c21-15-4-5-17-14(11-27-18(17)9-15)6-7-26-10-13-2-1-3-16(8-13)28-12-20(24,25)19(22)23;/h1-5,8-9,11,19,26-27H,6-7,10,12H2;1H |
| InChiKey | KXOQNPANAFXKTN-UHFFFAOYSA-N |
| CID | 21071391 |
| Short Description | 5-HT6 antagonist |
References
- J Arnt et al. Lu AE58054, a 5-HT6 antagonist, reverses cognitive impairment induced by subchronic phencyclidine in a novel object recognition test in rats. Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.
- KF Herrik et al. The 5-HT6 receptor antagonist idalopirdine potentiates the effects of acetylcholinesterase inhibition on neuronal network oscillations and extracellular acetylcholine levels.... Neuropharmacology. 2016 Mar 31;107:351-363.
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