Hydroxybupropion 是 Bupropion 的主要活性代谢物,是 nACh 受体的拮抗剂。 Hydroxybupropion 抑制去甲肾上腺素摄取 (IC50 = 1.7 μM)。
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Hydroxybupropion is the major active metabolite of Bupropion and an antagonist of nACh receptor. Hydroxybupropion inhibits norepinephrine uptake (IC50 = 1.7 μM).
体外活性
Hydroxybupropion shows stronger antitetrabenazine activity and has a lower LD50 value than the erythro- and threo- metabolites. Hydroxybupropion inhibits norepinephrine and dopamine uptake, antagonizes nicotine, and shows antidepressant effects in rodents[1].
Cas No.
92264-81-8
分子式
C13H18ClNO2
分子量
255.74
别名
Hydroxybupropione;Hydroxybupropion, (+/-)-;6-Hydroxybupropion
储存和溶解度
DMSO:90mg/mL (351.9mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years