Hydroxybupropion

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 IC₅₀ value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonist^[1] . IC50 & Target:IC50: 1.7 μM (Norepinephrine uptake)^[1]
nACh receptor^[1] In Vivo: 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^[1].