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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
Lu AE58054 hydrochloride (Idalopirdine) is a highly potent serotonin 5-HT6 receptor antagonist with reported Ki of 0.83 nM for human 5-HT6 and broad selectivity across more than 70 targets. It has good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. It potentiates donepezil (Axon 1438)-associated effects on neuronal oscillations and hippocampal acetylcholine levels.
The 5-HT6 receptor is implicated in cognition, cholinergic modulation and neuropsychiatric disease biology. Lu AE58054 is relevant for studying pro-cognitive serotonergic pharmacology and biomarker responses in CNS models.
Key Features
- Highly potent 5-HT6 receptor antagonist
- High selectivity across broad target panels
- Modulates cognition-associated pharmacodynamic biomarkers
- Potentiates donepezil effects in preclinical systems
Applications
- 5-HT6 receptor pharmacology
- Cognition and memory research
- Serotonergic-cholinergic interaction studies
- Schizophrenia and Alzheimer disease model assays
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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