CAS 92264-81-8: Hydroxybupropione

Hydroxybupropion (6-Hydroxybupropion) is the major active metabolite of Bupropion and an antagonist of nACh receptor. Hydroxybupropion inhibits norepinephrine uptake (IC50 = 1.7 μM).

Hydroxybupropion is a drug that is used to treat depressive disorders. It acts as a nicotinic acetylcholine receptor antagonist and a dopamine uptake inhibitor, which increases the levels of dopamine in the brain. It is also an antidepressant with clinical response after oral administration. The plasma concentration-time curve of hydroxybupropion can be found by using both the conventional single-phase linear regression method and a nonlinear mixed effects model. This drug may interact with other drugs, such as antidepressants and antipsychotics, and has been shown to increase their levels in the blood stream. Hydroxybupropion also interacts with drugs that affect metabolism, such as α1-acid glycoprotein, or are taken up by the liver, such as acetylcholinesterase inhibitors. The chemical stability of hydroxybupropion can be determined by examining its stereoselectivity for acetylcholine receptors, which is dependent on pH.