Hydroxybupropion (Synonyms: BUPOH, OH-bupropion) |
Catalog No.GC20057
One-Click Copy Product Info
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Hydroxybupropion, a major metabolite of bupropion, inhibits norepinephrine (NE) uptake, with an IC50 value of 1.7µM.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | BUPOH, OH-bupropion | ||
| Formula | C13H18CINO2 | M.Wt | 255.74 |
| Solubility | DMSO : 100 mg/mL (391.02 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)