134564-82-2

134564-82-2 structure

Name: Befloxatone
Chemical Name: (5R)-5-(methoxymethyl)-3-[4-[(3R)-4,4,4-trifluoro-3-hydroxybutoxy]phenyl]-1,3-oxazolidin-2-one
CAS Number: 134564-82-2
Molecular Formula: C₁₅H₁₈F₃NO₅
Molecular Weight: 349.30200
Catalog: Signaling Pathways Neuronal Signaling Monoamine Oxidase
Create Date: 2018-03-25 08:00:00
Modify Date: 2024-01-03 22:25:52
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].

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

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.