Isocarboxazid 是不可逆的、非选择性的单胺氧化酶Monoamine Oxidase抑制剂,其在大鼠大脑中测得的IC50值为4.8 μM。
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Isocarboxazid has the formula 1-benzyl-2-(5-methyl-3-isoxazolylcarbonyl)hydrazine-isocarboxazid. It is a monoamine oxidase inhibitor.[2] It is used in the treatment of major depression, dysthymic disorder, atypical disorder, panic disorder and the phobic disorders.
体外活性
In vivo studies demonstrated isocarboxazid-driven inhibition of MAO in the brain, heart, and liver. The reduced MAO activity, caused by isocarboxazid, results in an increased concentration of serotonin, epinephrine, norepinephrine, and dopamine in storage sites throughout the central nervous system (CNS) and sympathetic nervous system. The increase of one or more monoamines is the basis for the antidepressant activity of MAO inhibitors like isocarboxazid.[1]
体内活性
In vitro studies demonstrated isocarboxazid-driven inhibition of MAO in the brain, heart, and liver. The reduced MAO activity, caused by isocarboxazid, results in an increased concentration of serotonin, epinephrine, norepinephrine, and dopamine in storage sites throughout the central nervous system (CNS) and sympathetic nervous system. The increase of one or more monoamines is the basis for the antidepressant activity of MAO inhibitors like isocarboxazid.[1]
Cas No.
59-63-2
分子式
C12H13N3O2
分子量
231.255
储存和溶解度
DMSO:198.9 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years