| Identification | Back Directory | [Name]
Befloxatone | [CAS]
134564-82-2 | [Synonyms]
503
MD-370
MD370503
MD-370503
MD 370503
Befloxatone
(R)-5-(methoxymethyl)-3-(4-((R)-4,4,4-trifluoro-3-hydroxybutoxy)phenyl)oxazolidin-2-one
2-Oxazolidinone, 5-(methoxymethyl)-3-[4-[(3R)-4,4,4-trifluoro-3-hydroxybutoxy]phenyl]-, (5R)- | [Molecular Formula]
C15H18F3NO5 | [MDL Number]
MFCD00871024 | [MOL File]
134564-82-2.mol | [Molecular Weight]
349.3 |
| Chemical Properties | Back Directory | [Melting point ]
101° | [alpha ]
D20 -11.5° (c = 1 in methylene chloride) | [Boiling point ]
447.3±45.0 °C(Predicted) | [density ]
1.326±0.06 g/cm3(Predicted) | [pka]
12.13±0.20(Predicted) |
| Hazard Information | Back Directory | [Uses]
Befloxatone is a selective and reversible inhibitor of monoamine oxidase A. A third line agent for the treatment of resistant depression. | [in vivo]
Befloxatone (0.75 mg/kg; i.p.; single dose) increases tissue levels of monoamines and decreases levels of their deaminating metabolites in rats[1].
Befloxatone (1 mg/kg; i.p.; single dose) induces elevated levels of dopamine and corticonorepinephrine in the extracellular striatum of rats, but not elevates levels of corticoserotonin[1].
Befloxatone (0.03-0.3 mg/kg; p.o.; single dose) effectively inhibits the firing rate of serotonergic neurons and partially reduces the firing of norepinephric neurons, but had no effect on the firing of dopaminergic neurons in rats[1].
Befloxatone (1.5 mg/kg; p.o.; single dose) does not enhance the pressor effect of the central active dose of oral tyramine and has a broad safety profile in rats[1].
| [IC 50]
MAO-A: 4 nM (IC50); MAO-B: 300 nM (IC50) |
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