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Befloxatone

Names

[ CAS No. ]:
134564-82-2

[ Name ]:
Befloxatone

[Synonym ]:
UNII-4H75PAD8M3
(R)-5-(methoxymethyl)-3-(p[(R)-4,4,4-trifluoro-3-hydroxybutoxy]phenyl)-2-oxazolidinone
BEFLOXATONE
(R)-5-(methoxymethyl)-3-(4-((R)-4,4,4-trifluoro-3-hydroxybutoxy)phenyl)-oxazolidin-2-one
Befloxatone (INN)

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase
Research Areas >> Neurological Disease

[Target]

MAO-A:4 nM (IC50)

MAO-B:300 nM (IC50)


[In Vitro]

Befloxatone (100 nM; 0-100 min) 可逆抑制大鼠脑匀浆中的 MAO-A 活性，60 min 后不再发挥抑制作用[1]。

[In Vivo]

Befloxatone (0.75 mg/kg; i.p.; single dose) 在大鼠中增加单胺的组织水平，并降低其脱氨基代谢物的水平[1]。 Befloxatone (1 mg/kg; i.p.; single dose) 可诱导大鼠细胞外纹状体多巴胺和皮质去甲肾上腺素水平升高，但不诱导皮质 5-羟色胺水平升高[1]。 Befloxatone (0.03-0.3 mg/kg; p.o.; single dose) 在大鼠中有效抑制血清素能神经元的放电速率，部分降低去甲肾上腺素能神经元的发射，对多巴胺能神经元的激发没有影响[1]。 Befloxatone (1.5 mg/kg; p.o.; single dose) 在大鼠中不会增强中心活性剂量口服酪胺的升压作用，具有广泛的安全性[1]。

[References]

[1]. Curet O, et al. Preclinical profile of befloxatone, a new reversible MAO-A inhibitor. J Affect Disord. 1998 Dec;51(3):287-303.  

Chemical & Physical Properties

[ Density]:
1.326g/cm3

[ Boiling Point ]:
447.3ºC at 760mmHg

[ Molecular Formula ]:
C15H18F3NO5

[ Molecular Weight ]:
349.30200

[ Flash Point ]:
224.3ºC

[ Exact Mass ]:
349.11400

[ PSA ]:
68.23000

[ LogP ]:
2.41530

[ Vapour Pressure ]:
8.73E-09mmHg at 25°C

[ Index of Refraction ]:
1.498

Related Compounds