Emedastine (fumarate)
(Synonyms: 富马酸依美斯汀；富马酸依美司丁) 目录号 : GC43598
A histamine H1 receptor antagonist
Cas No.:87233-62-3
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
Emedastine is a potent and selective histamine H1 receptor antagonist with 37,744-fold and 9,562-fold selectivity over H2 and H3, respectively (Kis = 1.3, 49,067, and 12,430 nM for H1, H2, and H3, respectively). It is selective for H1 receptors with less than 50% inhibition of α1-, α2-, and β1-adrenergic, dopamine D1 and D2, and serotonin 5-HT1 and 5-HT2 receptors at a concentration of 10 µM. It inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC50s = 1.6 and 2.9 nM, respectively). Emedastine inhibits histamine-stimulated cytokine secretion by primary HCECs, including IL-6, IL-8, and GM-CSF secretion (IC50s = 2.23, 3.42, and 1.50 nM, respectively). In guinea pigs, ocular application of emedastine 4 hours after histamine challenge inhibits vascular permeability with an ED50 value of 0.019% w/v. Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.
| Cas No. | 87233-62-3 | SDF | |
| 别名 | 富马酸依美斯汀；富马酸依美司丁 | ||
| Canonical SMILES | CN(CC1)CCCN1C2=NC3=CC=CC=C3N2CCOCC.OC(/C=C/C(O)=O)=O.OC(/C=C\C(O)=O)=O | ||
| 分子式 | C17H26N4O•2C4H4O4 | 分子量 | 534.6 |
| 溶解度 | DMSO: Slightly Soluble,Methanol: Slightly Soluble | 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 | 1.8706 mL | 9.3528 mL | 18.7056 mL |
| 5 mM | 0.3741 mL | 1.8706 mL | 3.7411 mL |
| 10 mM | 0.1871 mL | 0.9353 mL | 1.8706 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。
Randomized, double-masked, placebo-controlled comparison of the efficacy of Emedastine difumarate 0.05% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution in the human conjunctival allergen challenge model
Clin Ther 2002 Mar;24(3):409-16.PMID:11952024DOI:10.1016/s0149-2918(02)85042-1.
Background: Emedastine difumarate 0.05% ophthalmic solution and ketotifen fumarate 0.025% ophthalmic solution are 2 topical antiallergic agents available in the United States and other countries. Emedastine is indicated for the temporary relief of the signs and symptoms of allergic conjunctivitis. Ketotifen is indicated for the temporary relief of ocular itching caused by allergic conjunctivitis. Objective: The purpose of this study was to compare the efficacy of these agents in the temporary relief of ocular itching due to allergic conjunctivitis. The 2 agents were compared with each other and with placebo (artificial tears) using the conjunctival allergen challenge (CAC) model. Methods: This was a single-center, randomized, double-masked, placebo-controlled study. At visit 1, CAC was performed on eligible subjects to identify the dose required to elicit a positive allergic reaction. Subjects returned after 7 days for visit 2 to confirm the allergen dose. On day 14 (+/-3) of the study, enrolled subjects were randomized to 1 of 3 treatment groups: Emedastine in I eye and placebo in the other, ketotifen in 1 eye and placebo in the other, or Emedastine in 1 eye and ketotifen in the other. In 25 subjects, bilateral CAC was performed 5 minutes after study medication instillation. In a second group of 20 subjects, CAC was performed 15 minutes after medication instillation. Itching was graded according to a standardized 5-point scale (0 = none to 4 = severe itching) at 3, 5, and 10 minutes postchallenge. Differences in efficacy scores between treatments and versus placebo were compared using 2-sample t tests of equal variance. Results: A total of 45 patients (mean age, 41.2 years) received treatment: 16 received Emedastine in 1 eye and ketotifen in the other; 14 received Emedastine in 1 eye and placebo in the other; and 15 received ketotifen in 1 eye and placebo in the other. Both Emedastine and ketotifen significantly inhibited itching (P < 0.05) compared with placebo at all time points after the 5- and 15-minute CAC. Mean raw scores for the active treatments were not statistically different. The mean itching efficacy scores were also not statistically different between active treatments. No adverse events were reported in this study. Conclusion: The results of this study suggest that Emedastine and ketotifen are not significantly different with respect to anti-itching efficacy in the CAC model of acute allergic conjunctivitis.
Onset and duration of action of ketotifen 0.025% and Emedastine 0.05% in seasonal allergic conjunctivitis : efficacy after repeated pollen challenges in the vienna challenge chamber
Clin Drug Investig 2003;23(5):329-37.PMID:17535045DOI:10.2165/00044011-200323050-00003.
Objective: To compare the efficacy, onset and duration of action, and the safety of ketotifen fumarate 0.025% ophthalmic solution and Emedastine difumarate 0.05% ophthalmic solution in subjects with seasonal allergic conjunctivitis (SAC) induced by allergen exposure, using the Vienna Challenge Chamber model. Design and setting: This was a double-masked, randomised, comparative, crossover study conducted at an allergy outpatient clinic in Austria. Study participants: Subjects with an allergy to grass pollen were exposed to the allergen in a pollen chamber for 4 hours, followed by a 3-hour break and then a second exposure for 3 hours. Interventions: Study participants were randomised to a treatment sequence (ketotifen followed by Emedastine or Emedastine followed by ketotifen), receiving 1 drop per eye of ketotifen or Emedastine 2 hours after the initial allergen exposure in the pollen chamber. Outcomes: Individual and composite ocular, individual and composite nasal, and total (ocular + nasal) symptom complex scores were determined by repeated exposure to allergen 0-2 hours and 5-8 hours after dosing. Onset of action was defined as the time to the first observation of a 20% reduction from baseline in the composite ocular symptom score. Results: All 37 subjects enrolled completed the study. The median time to onset of action was 15 minutes for ketotifen and 30 minutes for Emedastine. This difference was significant using the generalised linear model (p = 0.048), but not for the log-rank test analysis. In the initial 2 hours post dose, ketotifen provided significantly greater relief of both composite ocular symptoms (p = 0.026) and total symptom complex (p = 0.014). Both medications were effective in reducing symptoms 5 to 8 hours after dosing. No adverse events were reported for either treatment. Conclusions: In the Vienna Challenge Chamber model, ketotifen and Emedastine both effectively alleviated ocular symptoms of SAC after single-dose administration. Ketotifen had a faster onset of action and provided better symptom relief than Emedastine during the first 2 hours after dosing. The rapid onset of action and symptom control make ketotifen a valuable treatment for SAC.
Efficacy of olopatadine HCI 0.1%, ketotifen fumarate 0.025%, epinastine HCI 0.05%, Emedastine 0.05% and fluorometholone acetate 0.1% ophthalmic solutions for seasonal allergic conjunctivitis: a placebo-controlled environmental trial
Acta Ophthalmol 2009 Aug;87(5):549-54.PMID:18631332DOI:10.1111/j.1755-3768.2008.01265.x.
Purpose: We aimed to compare the clinical efficacy and ocular surface variables of olopatadine, ketotifen fumarate, epinastine, Emedastine and fluorometholone acetate ophthalmic solutions in preventing the signs and symptoms of seasonal allergic conjunctivitis (SAC). Methods: This was a prospective, randomized, double-blinded and placebo-controlled study. A total of 100 patients with SAC were randomly assigned to one of five groups, in which they were administered olopatadine, ketotifen fumarate, epinastine, Emedastine or fluorometholone acetate, instilled twice daily for 2 weeks. One eye of each patient was treated with the study drug and the other was treated with a placebo. Signs and symptoms of allergic conjunctivitis (itching, redness, tearing, chemosis and eyelid swelling) were scored on a 4-point scale. Each symptom was assessed at baseline and then again after 1 and 2 weeks of treatment. Ocular surface variables were assessed by conjunctival impression cytology. Results: At weeks 1 and 2, all antiallergic agents were significantly more effective than placebo in alleviating itching, redness, tearing, chemosis and eyelid swelling. Fluorometholone acetate was significantly less effective than the other agents in reducing itching and redness at all control visits. Ocular surface findings by impression cytology improved significantly after all treatments compared with placebo. Conclusions: In patients with SAC, olopatadine, ketotifen, epinastine and Emedastine are more efficacious than fluorometholone acetate in preventing itching and redness. All the antiallergic agents gave similar results in terms of reducing tearing, chemosis and eyelid swelling. Our data showed that impression cytology parameters improved after treatment with antiallergic agents in patients with SAC.
[Anti-allergic effects of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole fumarate (KB-2413)]
Nihon Yakurigaku Zasshi 1987 Feb;89(2):55-62.PMID:2883094DOI:10.1254/fpj.89.55.
The effects of KB-2413 on four types of allergic reactions classified by Coombs and Gell were investigated. KB-2413 inhibited homologous passive cutaneous anaphylaxis and passive anaphylactic bronchoconstriction in guinea pigs mediated by IgE-like antibody, and ED50 values were 0.0017 mg/kg, p.o., and 0.022 mg/kg, p.o., respectively. KB-2413 also inhibited IgG-mediated anaphylactic bronchoconstriction in guinea pigs actively sensitized with egg albumin. Both complement-dependent immune hemolysis and complement-independent hypotonic hemolysis were inhibited by KB-2413 in a concentration-dependent manner. KB-2413 had no effect on the Forssman systemic reaction. The passive Arthus reaction in guinea pigs sensitized with anti-egg albumin rabbit serum was unaffected by KB-2413. However, the early stage of the active Arthus reaction in rabbits sensitized with egg albumin was inhibited. KB-2413 had an inhibitory effect on the efferent phase of delayed-type hypersensitivity induced by picryl chloride (PC-DTH) in mice. On the other hand, the afferent phase of PC-DTH in mice was unaffected. These results suggest that KB-2413 strongly suppresses type I allergic reactions, and it slightly suppresses type II, III and IV allergic reactions.