Hydroxybupropion 是 Bupropion 的主要活性代谢产物，主要是通过 CYP2B6 代谢的。Bupropion 是一种非典型的抗抑郁剂和戒烟剂。Hydroxybupropion 抑制去甲肾上腺素 (norepinephrine uptake) 的摄取，IC₅₀ 值为 1.7 μM。Hydroxybupropion 也是一种 nACh 受体拮抗剂。

Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6. Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC 50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist .

Solid

IC50: 1.7 μM (Norepinephrine uptake)
nACh receptor

Plasma levels of Hydroxybupropion greatly exceed those of the parent drug, reaching 10 to 100 times the concentration of Bupropion. Hydroxybupropion shows stronger antitetrabenazine activity (indicative of an antidepressant activity in animals) and has a lower LD50 value than the erythro- and threo- metabolites, suggesting that Hydroxybupropion is the most important active metabolite in vivo for its antidepressant activity. Hydroxybupropion is pharmacologically active, inhibiting norepinephrine and dopamine uptake, and antagonizing nicotine and showing antidepressant effects in rodents. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Damaj MI, et al. Enantioselective effects of hydroxy metabolites of bupropion on behavior and on function of monoamine transporters and nicotinic receptors. Mol Pharmacol. 2004 Sep;66(3):675-82.

In Vitro: DMSO : 100 mg/mL (391.02 mM; Need ultrasonic)配制储备液