| Identification | Back Directory | [Name]
LUSAPERIDONE | [CAS]
214548-46-6 | [Synonyms]
R107474
LUSAPERIDONE
Lusaperidone [inn]
4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-(3,4-dihydrobenzofuro[3,2-c]pyridin-2(1H)-yl)ethyl]-2-methyl-
2-Methyl-3-[2-(1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridin-2-yl)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one | [Molecular Formula]
C22H21N3O2 | [MDL Number]
MFCD09837832 | [MOL File]
214548-46-6.mol | [Molecular Weight]
359.42 |
| Chemical Properties | Back Directory | [Boiling point ]
538.3±60.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
6.93±0.20(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Lusaperidone (R107474) is an α2 adrenergic receptor antagonist with Kis of 0.13 and 0.15 nM for α2A and α2C, respectively. | [in vivo]
Lusaperidone occupies the α2A and α2C adrenergic receptor with an ED50 of 0.014 mg/kg sc (0.009-0.019) and 0.026 mg/kg sc (0.022-0.030), respectively. The uptake of R107474 after in vivo intravenous administration is very rapid; in most tissues (including the brain) it reaches maximum concentration at 5 min after tracer injection[1]. | [References]
[1] Van der Mey M, et al. Synthesis and biodistribution of [11C]R107474, a new radiolabeled alpha2-adrenoceptor antagonist. Bioorg Med Chem. 2006 Jul 1;14(13):4526-34. DOI:10.1016/j.bmc.2006.02.029 |
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