| Identification | Back Directory | [Name]
Lu AE 58054 Hydrochloride | [CAS]
467458-02-2 | [Synonyms]
CS-1517
IdalopirdineHCl
Lu AE58054(HCl)
Lu AE58054 HCl salt
Lu AE 58054 Hydrochloride
Lu AE58054 (Hydrochloride)
Idalopirdine Hydrochloride
LU AE58054; LU AE-58054; LU AE 58054; IDALOPIRDINE HYDROCHLORIDE; LU AE 58054 HYDROCHLORIDE
6-fluoro-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]-1H-Indole-3-ethanamine hydrochloride
N-[2-(6-Fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine monohydrochloride
2-(6-Fluoro-1H-indol-3-yl)-N-[3-(2,2,3,3-tetrafluoropropoxy)benzyl]ethanamine hydrochloride (1:1) | [Molecular Formula]
C20H20ClF5N2O | [MDL Number]
MFCD25372046 | [MOL File]
467458-02-2.mol | [Molecular Weight]
434.831 |
| Hazard Information | Back Directory | [Uses]
Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders[1][2]. | [in vivo]
Idalopirdine (intraperitoneal injection, 5?mg/kg, daily, 28 days) hydrochloride can reduce food intake and body weight in over-eating rat models[1].
Idalopirdine (1 or 2?mg/kg, i.v) hydrochloride can dose-dependently increase the gamma power during nPO electrical stimulation, enhance effect of donepezil on cortical gamma oscillations but no alteration of sleep-wake patterns in rats[2].
| Animal Model: | Male Wistar rats[1] | | Dosage: | 5?mg/kg | | Administration: | intraperitoneal injection, daily, 28 days | | Result: | Significantly reduced the amount of calories consumed by animals in a palatable diet and significantly reduced plasma levels of glucose, triglycerides and cholesterol. |
| Animal Model: | Male Sprague-Dawley rats[2] | | Dosage: | 1 or 2?mg/kg | | Administration: | i.v. | | Result: | No significant increase in the gamma power at 1 mg/kg and significantly increased the gamma power at 2 mg/kg.
Significantly enhanced and/or prolonged effect of low-dose donepezil (0.3 mg/kg) on gamma power during 60-minute nPO stimulation after donepezil administration. |
| [IC 50]
5-HT6 Receptor: 0.83 nM (Ki) | [storage]
Store at -20°C | [References]
[1] Magdalena Kotańska, et al. Idalopirdine, a selective 5-HT6?receptor antagonist, reduces food intake and body weight in a model of excessive eating. Metab Brain Dis. 2018 Jun;33(3):733-740. DOI:10.1007/s11011-017-0175-1
[2] Maria Amat-Foraster, et al. The 5-HT6?receptor antagonist idalopirdine potentiates the effects of donepezil on gamma oscillations in the frontal cortex of anesthetized and awake rats without affecting sleep-wake architecture. Neuropharmacology. 2017 Feb;113(Pt A):45-59. DOI:10.1016/j.neuropharm.2016.09.017 |
|
|