| Identification | Back Directory | [Name]
1H-Indole-3-ethanaMine, 6-fluoro-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]Methyl]- | [CAS]
467459-31-0 | [Synonyms]
LU AE58054
LU AE58084
idalopirdine
LU AE58054(Idalopirdine)
Idalopirdine(Lu-AE-58054)
IDALOPIRDINE;LU AE 58054;LUAE58054
LU AE58054 HYDROCHLORIDE; LU AE 58054 HYDROCHLORIDE
N-[2-(6-Fluoro-1H-indol-3-yl)ethyl]-3-(2,2,3,3-tetrafluoropropoxy)benzylamine
6-fluoro-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]-1H-Indole-3-ethanamine
1H-Indole-3-ethanaMine, 6-fluoro-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]Methyl]-
2-(6-fluoro-1H-indol-3-yl)-N-[[3-(2,2,3,3-tetrafluoropropoxy)phen yl]methyl]ethanamine | [Molecular Formula]
C20H19F5N2O | [MDL Number]
MFCD18633269 | [MOL File]
467459-31-0.mol | [Molecular Weight]
398.37 |
| Chemical Properties | Back Directory | [Boiling point ]
500.9±50.0 °C(Predicted) | [density ]
1.309±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
25℃: DMSO | [form ]
Powder | [pka]
16.63±0.30(Predicted) | [color ]
white to beige | [InChI]
1S/C20H19F5N2O/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 | [InChIKey]
YBAWYTYNMZWMMJ-UHFFFAOYSA-N | [SMILES]
FC(F)(C(F)F)COc1cc(ccc1)CNCCc2c3c([nH]c2)cc(cc3)F |
| Hazard Information | Back Directory | [Uses]
The selective and high affinity 5-?HT6 receptor antagonist Lu AE58054 as promising treatment for cognitive disorders, in particular for Alzheimer’s disease (AD). | [Biological Activity]
Idalopirdine (Lu AE58054) is an orally availableand potent antagonist of the serotonin 6 (5-HT6) receptor. Idalopirdine has been reported to be highly selective over other G-protein coupled receptors. It has K(d) of 0.2nM for the 5-HT6 receptor with 16-fold selectivity over the 5-HT2A receptor (K(i) 3.2nM) and >100-fold selectivity to all other evaluated targets. | [in vivo]
Idalopirdine (intraperitoneal injection, 5?mg/kg, daily, 28 days) can reduce food intake and body weight in over-eating rat models[1].
Idalopirdine (1 or 2?mg/kg, i.v) 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) |
|
| Company Name: |
Spectrum Chemical Manufacturing Corp.
|
| Telephone: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|