| CAS NO: | 467458-02-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 434.83 |
|---|---|
| Formula | C20H20ClF5N2O |
| CAS No. | 467458-02-2 (HCl); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 10 mM in DMSO |
| Water: <1 mg/mL | |
| Ethanol: | |
| SMILES Code | FC1=CC(NC=C2CCNCC3=CC(OCC(F)(F)C(F)F)=CC=C3)=C2C=C1.Cl |
| Synonyms | Lu AE58054 Hydrochloride; Idalopirdine Hydrochloride |
| In Vitro | In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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 with phencyclidine (PCP 2 mg/kg b.i.d., i.p. for 7 d, followed by 7 d drug free). The results indicate that Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia |
| Animal model | Rat |
| Formulation & Dosage | 5-20 mg/kg; p.o |
| References | Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.Eur J Pharmacol. 2012 Feb 15;676(1-3):6-11. |
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