1. Neuronal Signaling
  2. Monoamine Oxidase
  3. Befloxatone

Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential.

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Befloxatone Chemical Structure

Befloxatone Chemical Structure

CAS No. : 134564-82-2

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Description

Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential[1].

IC50 & Target[1]

MAO-A

4 nM (IC50)

MAO-B

300 nM (IC50)

In Vitro

Befloxatone (100 nM; 0-100 min) reversibly reduces MAO-A activity in rat brain homogenates, while completely lost 60 min later[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

349.30

Formula

C15H18F3NO5

CAS No.
Unlabeled CAS

SMILES

O=C1O[C@@H](COC)CN1C2=CC=C(OCC[C@@H](O)C(F)(F)F)C=C2

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Befloxatone Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Befloxatone
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HY-120017
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