Befloxatone

Modify Date: 2024-01-03 22:25:52

Befloxatone Structure
Befloxatone structure
Common Name Befloxatone
CAS Number 134564-82-2 Molecular Weight 349.30200
Density 1.326g/cm3 Boiling Point 447.3ºC at 760mmHg
Molecular Formula C15H18F3NO5 Melting Point N/A
MSDS N/A Flash Point 224.3ºC

 Use of 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[1].

 Names

Name (5R)-5-(methoxymethyl)-3-[4-[(3R)-4,4,4-trifluoro-3-hydroxybutoxy]phenyl]-1,3-oxazolidin-2-one
Synonym More Synonyms

 Befloxatone 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
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

 Synonyms

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)