Hydroxy Bupropion, a major metabolite of bupropion, inhibits norepinephrine (NE) uptake with an IC50 value of 1.7μM [1]. Hydroxy Bupropion can inhibit the function of 5-HT3A receptors in oocytes and suppress the 5-HT 3A receptor-mediated serotonin-gated currents, with the IC50 value of 112μM [2]. The metabolic level and clearance rate of Hydroxy Bupropion can be used to assess the CYP2B6 activity in glomerular diseases[3]. Hydroxy Bupropion is widely used as an internal standard to optimize the solid-phase extraction-liquid chromatography-tandem mass spectrometry analysis conditions, enabling efficient analysis of the relevant metabolites in plasma and urine[4].
References:
[1] Damaj M I, Carroll F I, Eaton J B, et al. Enantioselective effects of hydroxy metabolites of bupropion on behavior and on function of monoamine transporters and nicotinic receptors[J]. Molecular pharmacology, 2004, 66(3): 675-682.
[2] Pandhare A, Pappu A S, Wilms H, et al. The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors[J]. Neuropharmacology, 2017, 113: 89-99.
[3] Joy M S, Frye R F, Stubbert K, et al. Use of enantiomeric bupropion and hydroxybupropion to assess CYP2B6 activity in glomerular kidney diseases[J]. Journal of clinical pharmacology, 2010, 50(6): 714.
[4] Coles R, Kharasch E D. Stereoselective analysis of bupropion and hydroxybupropion in human plasma and urine by LC/MS/MS[J]. Journal of Chromatography B, 2007, 857(1): 67-75.
Hydroxy Bupropion是bupropion的主要代谢产物，可抑制去甲肾上腺(NE)摄取，IC50值为1.7μM[1]。Hydroxy Bupropion可抑制卵母细胞中5-HT3A受体的功能，并抑制5-HT3A受体介导的血清素门控电流，IC50值为112μM[2]。Hydroxy Bupropion的代谢水平和清除率可用于评估肾小球疾病中的CYP2B6活性[3]。Hydroxy Bupropion被广泛用作内标，以优化固相萃取-液相色谱-串联质谱分析条件，从而高效分析血浆和尿液中的相关代谢物[4]。