Hydroxybupropion, a major metabolite of bupropion, inhibits norepinephrine (NE) uptake, with an IC50 value of 1.7µM[1]. Hydroxybupropion blocks the development of nicotine-induced conditioned place preference[2]. Hydroxybupropion has been widely used as a model compound for the development of novel quantitative assays to identify related compounds in plasma[3].
In vivo, Hydroxybupropion treatment via subcutaneous injection at a single dose of 10mg/kg for 30min inhibited the acquisition of nicotine reward and reversed affective and somatic withdrawal signs in nicotine-dependent mice[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] Zhu A Z X, Cox L S, Nollen N, et al. CYP2B6 and bupropion's smoking‐cessation pharmacology: the role of hydroxybupropion[J]. Clinical Pharmacology & Therapeutics, 2012, 92(6): 771-777.
[3] Masters A R, McCoy M, Jones D R, et al. Stereoselective method to quantify bupropion and its three major metabolites, hydroxybupropion, erythro-dihydrobupropion, and threo-dihydrobupropion using HPLC–MS/MS[J]. Journal of Chromatography B, 2016, 1015: 201-208.
[4] Damaj M I, Grabus S D, Navarro H A, et al. Effects of hydroxymetabolites of bupropion on nicotine dependence behavior in mice[J]. The Journal of pharmacology and experimental therapeutics, 2010, 334(3): 1087-1095.
Hydroxybupropion是安非他酮的主要代谢产物，可抑制去甲肾上腺素的摄取，IC50值为1.7µM[1]。Hydroxybupropion可阻断尼古丁诱导的条件性位置偏好的形成[2]。Hydroxybupropion已被广泛用作模型化合物，用于开发新型定量分析方法以检测血浆中相关物质[3]。
在体内，单次皮下注射10mg/kg剂量的Hydroxybupropion 30分钟，可抑制尼古丁依赖小鼠对尼古丁奖赏效应的获取，并逆转戒断过程中的情感与躯体症状[4]。