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。
Cas No.:92264-81-8
Sample solution is provided at 25 µL, 10mM.
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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]。
| Animal experiment [1]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Male C57BL/6J mice were housed in a 21°C humidity-controlled facility with food and water available ad libitum. The rooms were on a 12-h light/dark cycle (lights on at 7:00 AM). Mice were anesthetized with sodium pentobarbital (45mg/kg; i.p.) and implanted with osmotic minipumps filled with nicotine or saline solution. For withdrawal studies, mice received 36mg/kg/day for 14 days. Minipumps were removed on the evening of day 14, and testing was initiated on day 15, approximately 18 to 24h after minipump removal. Mice were then injected subcutaneously with a single dose of vehicle, bupropion, and Hydroxybupropion (10mg/kg) for 30min. The mice were evaluated for 5min in the plus maze test for anxiety-related behavior, followed by a 20-min observation of somatic signs. |
Dosage form | 10mg/kg for once; s.c. |
Applications | Hydroxybupropion treatment reversed affective and somatic withdrawal signs in nicotine-dependent mice. |
References: | |
| Cas No. | 92264-81-8 | SDF | |
| 别名 | 羟基安非他酮 | ||
| 分子式 | C13H18CINO2 | 分子量 | 255.74 |
| 溶解度 | DMSO : 100 mg/mL (391.02 mM; Need ultrasonic) | 储存条件 | -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9102 mL | 19.5511 mL | 39.1022 mL |
| 5 mM | 782 μL | 3.9102 mL | 7.8204 mL |
| 10 mM | 391 μL | 1.9551 mL | 3.9102 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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