Bioactivity | 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]. |
Invitro | 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]。 |
Name | Befloxatone |
CAS | 134564-82-2 |
Formula | C15H18F3NO5 |
Molar Mass | 349.30 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Curet O, et al. Preclinical profile of befloxatone, a new reversible MAO-A inhibitor. J Affect Disord. 1998 Dec;51(3):287-303. |