Medifoxamine
(Synonyms: 姜地汐名) 目录号 : GC63578
Medifoxamine 是一种抑制单胺再摄取的抗抑郁药物，优先抑制多巴胺再摄取 (dopamine reuptake)。
Cas No.:32359-34-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Medifoxamine is a monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake[1].
[1]. Saleh S, et al. Ocular hypotensive effects of medifoxamine. Br J Clin Pharmacol. 1992;34(3):269-271.
| Cas No. | 32359-34-5 | SDF | |
| 别名 | 姜地汐名 | ||
| 分子式 | C16H19NO2 | 分子量 | 257.33 |
| 溶解度 | DMSO : 100 mg/mL (388.61 mM; Need ultrasonic) | 储存条件 | Store at -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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8861 mL | 19.4303 mL | 38.8606 mL |
| 5 mM | 0.7772 mL | 3.8861 mL | 7.7721 mL |
| 10 mM | 0.3886 mL | 1.943 mL | 3.8861 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
New statistical proposals to evaluate the benefit/risk ratio of long-term treatment of depression: application to a one-year double-blind study comparing Medifoxamine with fluoxetine
Clin Drug Investig 1998;15(4):285-95.PMID:18370483DOI:10.2165/00044011-199815040-00004.
The aim of this study was to determine the benefit/risk ratio of long-term treatment with Medifoxamine, a non-tricyclic, non-monoamine oxidase inhibitor agent, and fluoxetine in patients with acute depressive episode and at high risk of relapse and/or recurrence. The study involved a 12-month double-blind, randomised, parallel-group design with a multicentric trial setting conducted by 64 participating physicians. 155 and 158 patients of either gender, aged between 18 and 70 years, were allocated to fluoxetine and Medifoxamine, respectively. All patients had an acute depressive episode defined by the presence of at least five of the DSM III-R criteria with a minimal score of 25 on the Montgomery and Asberg Depression Rating Scale (MADRS). All subjects had at least one previous documented depressive episode in their medical history. The main outcome criterion consisted of good therapeutic response defined by a sustained 50% reduction of the Clinical Global Impression (CGI) score combined with the absence of any serious or troublesome (i.e. intensity motivating study discontinuation) events. In the fluoxetine and Medifoxamine groups, respectively, 45.2% and 43% of the randomised patients completed the 12-month follow-up period with no major differences between groups regarding the reasons for treatment withdrawal. With each treatment 58% of the patients reached at least a 50% decrease in their CGI score, with no differences on the evolution of the MADRS, Hamilton Anxiety Rating Scale (HARS), the Self Rating Depression Scale of Zung (Zung scale) and Scott depression visual analogue scale (VAS) scores on average. According to the main efficacy criterion, 26% of the patients in the fluoxetine group were considered as responders compared with 36% in the Medifoxamine group (p = 0.047). When only serious adverse effects were considered in combination with CGI scores to define response rates, the respective percentages were in favour of Medifoxamine but the difference (45 vs 53%) was not significant. Results with Medifoxamine were better in the elderly whereas, with fluoxetine, best responses were observed in younger patients. In conclusion, Medifoxamine was an active and well tolerated drug in the continuation and maintenance treatment of depression. Its benefit/risk ratio appeared to be superior to fluoxetine, but this difference was mainly based on the occurrence of less minor adverse effects, a potential advantage not sufficient to favour better compliance with long-term therapy. Nevertheless, efficacy and tolerance of Medifoxamine merits further evaluation in specific elderly populations.
The pharmacokinetics and pharmacodynamics of Medifoxamine after oral administration in healthy elderly volunteers
Eur J Clin Pharmacol 1994;46(2):163-6.PMID:8039537DOI:10.1007/BF00199882.
The pharmacokinetics and psychomotor effects of Medifoxamine, a 5 HT reuptake inhibitory antidepressant, were studied in healthy elderly volunteers after single and multiple dosing. The elimination half life (t1/2z) after single doses of 300 mg was 2.8 h--almost identical to that found in young volunteers. After seven days of dosing at 100 mg three times daily the mean corrected AUC after 300 mg significantly increased from 1.04 to 1.34 mg.h.l-1 and t1/2z increased to 4.0 h (NS). There were no significant changes in critical flicker fusion frequency, symbol digit substitution, continuous attention or choice reaction times.
Ocular hypotensive effects of Medifoxamine
Br J Clin Pharmacol 1992 Sep;34(3):269-71.PMID:1389953DOI:10.1111/j.1365-2125.1992.tb04136.x.
Medifoxamine is a novel monoamine re-uptake inhibiting antidepressive drug which preferentially inhibits dopamine reuptake. In human volunteer studies it has been found to reduce significantly intraocular pressure after single oral doses of 300-1000 mg, and to produce a small but statistically significant miosis. Its maximal ocular hypotensive action was less than that of oral timolol 20 mg.
Absolute bioavailability and pharmacokinetics of Medifoxamine in healthy humans
Br J Clin Pharmacol 1990 Oct;30(4):621-4.PMID:2291875DOI:10.1111/j.1365-2125.1990.tb03823.x.
Medifoxamine is a new monoamine re-uptake inhibiting antidepressant drug. Twelve volunteers received 100 mg by i.v. infusion over 15 min and 500 mg by mouth fasting. The treatments were given 1 week apart in a randomised cross-over design. Venous blood samples (10 ml) were taken at intervals for 24 h for h.p.l.c. measurement of serum Medifoxamine. A biexponential decline of serum Medifoxamine concentration was observed after intravenous administration in all subjects and similar terminal elimination half-lives were observed following both routes, indicating that oral absorption is not rate-limiting. The absolute bioavailability of oral Medifoxamine was 21%.
Spectrofluorimetric analysis and buccal absorption of Medifoxamine
J Pharm Pharmacol 1986 Aug;38(8):629-30.PMID:2876086DOI:10.1111/j.2042-7158.1986.tb03098.x.
Medifoxamine is a new investigational antidepressant drug. Its buccal absorption at pH 5-9, which can be considered as an in-vivo model of passive drug transfer through a lipid membrane, was studied in six normal, healthy volunteers to predict its pharmacokinetic profile in man. Maximum absorption of Medifoxamine occurred at pH 8, which is close to its pKa (8.5).