Dimethindene maleate
目录号 : GC66445
Dimethindene maleate 是一种选择性的 histamine H1 拮抗剂，具有抗组胺效应。Dimethindene maleate 可用于过敏性反应的研究。
Cas No.:3614-69-5
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
Dimethindene maleate is a selective histamine H1 antagonist with antihistamine effects. Dimethindene maleate can be used for the research of hypersensitivity reactions[1][2][3].
Dimethindene maleate (1-1000 μM) suppresses the cromakalim-induced/glibenclamide-sensitive K＋ currents in a concentration-dependent and reversible manner with an IC50 value of 29.5 μM[2].
Dimethindene maleate (1-1000 μM) inhibits Y-26763-induced glibenclamide-sensitive K＋ currents with an IC50 value of 49 μM[2].
Dimethindene maleate (0.25 mg; i.p. once) affects wound healing in mice[1].
| Animal Model: | C57BL/6 mice with wound healing[1] |
| Dosage: | 0.25 mg |
| Administration: | Intraperitoneal injection; 0.25 mg once |
| Result: | Significantly delayed skin wound and only showed wound closure impairment in the initial phase wound healing. |
| Cas No. | 3614-69-5 | SDF | Download SDF |
| 分子式 | C24H28N2O4 | 分子量 | 408.49 |
| 溶解度 | DMSO : 125 mg/mL (306.01 mM; Need ultrasonic) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 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 | 2.448 mL | 12.2402 mL | 24.4804 mL |
| 5 mM | 0.4896 mL | 2.448 mL | 4.8961 mL |
| 10 mM | 0.2448 mL | 1.224 mL | 2.448 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。
Comparative effect of Dimethindene maleate and chlorpheniramine maleate on histamine-induced weal and flare
J Int Med Res 1991 Nov-Dec;19(6):479-83.PMID:1773908DOI:10.1177/030006059101900608.
Antihistaminic activity of 3 or 6 mg Dimethindene maleate was compared with that of placebo and 12 mg chlorpheniramine maleate in 60 healthy volunteers in a randomized, crossover study. Activity of each drug was assessed by measuring 2 micrograms histamine-induced weal and flare areas. Compared with placebo, both doses of dimethindene and chlorpheniramine significantly (P less than 0.001) reduced weal area. Both doses of dimethindene (P less than 0.001) and chlorpheniramine (P less than 0.05) also significantly reduced flare area. Dimethindene (6 mg) brought about the maximum reduction in weal area (28.8%) and flare area (39.1%). Dimethindene (6 mg) also reduced weal area significantly (P less than 0.01) compared with chlorpheniramine and reduced flare area significantly (P less than 0.05) compared with 3 mg dimethindene. Using a 100 mm visual analogue scale for assessment of weal and flare intensities, 6 mg dimethindene again produced the maximum response. The study confirmed that the antihistamine activity of dimethindene was better than that of chlorpheniramine.
Dimethindene maleate in the treatment of pruritus caused by varizella zoster virus infection in children
Arzneimittelforschung 1997 Nov;47(11):1233-5.PMID:9428981doi
The efficacy and tolerability of Dimethindene maleate (CAS 3614-69-5, DMM, Fenistil) as drops in the treatment of pruritus in children suffering from chicken-pox were investigated in a study with two different doses of Dimethindene maleate and placebo. 128 children, 1 to 6 years of age, were included in a double blind, randomized, placebo controlled, multi-center clinical trial. Patients received either a dosage of DMM of 0.1 mg/kg x d, or 0.05 mg/kg x d, or placebo, respectively. All patients received a commercially available astringent lotion for topical treatment of skin lesions. The primary efficacy criterion which was the change in the itching severity score from baseline to the end of the treatment assessed as area under the baseline (AUB) showed for both treatments with DMM a statistically significant superiority versus placebo in reducing the severity of itching. There was no statistically proven difference between the two verum groups.
Effect-kinetic characterization of Dimethindene maleate following oral administration (Fenistil, Tropfen)
Fundam Clin Pharmacol 1990;4(6):673-83.PMID:2096106DOI:10.1111/j.1472-8206.1990.tb00047.x.
Dimethindene maleate is a well known H1-receptor antagonist with strong affinity to the H1-receptor. In order to evaluate the time course of its activity, Dimethindene maleate was investigated in a histamine provocation model in man. Eight healthy male volunteers were treated either with 4 mg Dimethindene maleate using a commercially available solution (Fenistile, Tropfen) or an identically appearing placebo solution (po) following a double-blind, crossover study design. Intracutaneous histamine injections were administered at -1, 2, 5, 14, 17, 20, 23, 26 and 29 h following drug administration. Areas of flares and weals were measured 5, 10, 20, and 30 min following histamine provocation. A strong inhibition of the development of flares and weals was observed to be more pronounced in flares than in weals. Baseline adjusted areas under the curve differ statistically significantly following verum and placebo treatment conditions (P = 0.0028). According to the time schedule of the study maximal effects were observed at time point 5 h. The mean residence times of the inhibitory effects were calculated to be congruent to 13 h compared to the mean residence times of dimethindene blood levels of approximately 8 h indicating a non-linear relationship between blood level and effect.
Dimethindene maleate in the treatment of sunburn. A double-blind, placebo-controlled pilot study
Arzneimittelforschung 1999 Apr;49(4):374-9.PMID:10337458DOI:10.1055/s-0031-1300429.
The efficacy of topical Dimethindene maleate (DMM, CAS 31614-69-5, Fenistil Gel) in the treatment of sunburn was evaluated in a placebo-controlled, 1-period crossover trial in 24 healthy volunteers. An UV-erythema (sunburn) of a well-defined intensity and extent was experimentally induced on three different skin test-areas by means of UV-A/B irradiation with three times the minimal erythema dose (MED). About 24 h after irradiation, one skin test-area was subjected to a 1-h occlusive treatment with DMM gel, the second test area was subjected to treatment with a placebo gel and the third one remained untreated. As objective-quantitative indicators of tenderness, a key symptom of sunburn, sensory and pain thresholds to CO2-Laser stimulation and laser somatosensory evoked potentials (SEPs) in Vertex-EEG were assessed about 1.5 h postdose. The reaction times (RTs) to painless and painful CO2-laser stimulation (sensory and pain threshold level, respectively) on the DMM-treated area were significantly longer than RTs to stimulation on the placebo-treated area. Thresholds in terms of laser energy showed no differences between the treatments. The SEP N1-amplitude on the DMM-area was markedly decreased in comparison to placebo. With regard to subjective sensations of pain, itching and tenderness assessed by means of visual analogue scales (VAS), no clinically relevant differences between treatments were observed after sole UV-irradiation. After additional laser stimulation tenderness was--objectively but not subjectively--decreased on the DMM-area versus placebo. Both gel preparations were well tolerated.
The effect of topical Dimethindene maleate on weal reactions
Br J Clin Pharmacol 1987 Feb;23(2):234-6.PMID:2881575DOI:10.1111/j.1365-2125.1987.tb03035.x.
The topical effect of the histamine H1-receptor antagonist Dimethindene maleate on the wealing response to intradermal histamine, compound 48/80 and house dust mite antigen was studied in 16 subjects using a double-blind procedure. The mean reduction in weal area +/- s.e. mean was 44% +/- 13%, 43% +/- 13% and 31% +/- 13% for histamine, 48/80 and antigen respectively. We conclude that Dimethindene maleate is a moderately potent H1-receptor antagonist, and that the inhibition of the 48/80 and house dust mite induced weals is accounted for by the antihistaminic effect of Dimethindene maleate.