Bepotastine
(Synonyms: 贝他斯汀) 目录号 : GC39479
A histamine H1 receptor antagonist
Cas No.:125602-71-3
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
Bepotastine is an antagonist of the histamine H1 receptor that is selective over H3, α1-, α2-, and β-adrenergic, dopamine D2long, serotonin 5-HT2, muscarinic acetylcholine, and benzodiazepine receptors.1 It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED50 = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED50 = 3.2 ?g/kg).2,3 Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner.4 Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.
1.Kato, M., Nishida, A., Aga, Y., et al.Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergic agent betotastine besilate.Arzneimittelforschung.47(10)1116-1124(1997) 2.Murata, T., Matsumoto, Y., Suzuki, T., et al.Effect of betotastine besilate (TAU-284), a novel anti-allergic agent, on experimental allergic rhinitisArerugi46(7)576-584(1997) 3.Matsubara, S., Ono, C., Yamazaki, N., et al.Inhibitory effects of bepotastine, a novel anti-allergic drug on histamine-induced bronchoconstriction in anesthetized dogsYakuri to Chiryo25(4)895-900(1997) 4.Kida, T., Fuji, A., Sakai, O., et al.Bepotastine besilate, a highly selective histamine H1 receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis modelsExp. Eye Res.91(1)85-91(2010)
| Cas No. | 125602-71-3 | SDF | |
| 别名 | 贝他斯汀 | ||
| Canonical SMILES | O=C(O)CCCN1CCC(O[C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=N3)CC1 | ||
| 分子式 | C21H25ClN2O3 | 分子量 | 388.89 |
| 溶解度 | DMSO : 78mg/mL; Water : 30mg/mL (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 | 2.5714 mL | 12.8571 mL | 25.7142 mL |
| 5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL |
| 10 mM | 0.2571 mL | 1.2857 mL | 2.5714 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。
Oral Bepotastine: in allergic disorders
Drugs 2010 Aug 20;70(12):1579-91.PMID:20687621DOI:10.2165/11205880-000000000-00000.
Oral Bepotastine is a second-generation histamine H(1) receptor antagonist that also suppresses some allergic inflammatory processes. Numerous short- and long-term clinical trials and surveillance studies have shown that twice-daily Bepotastine is an effective and generally well tolerated antihistamine in the treatment of patients with allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus). Bepotastine 20 mg/day was significantly more effective than terfenadine 120 mg/day in patients with perennial allergic rhinitis, as evaluated by the final global improvement rating and several other endpoints in a phase III trial. In phase III trials in patients with chronic urticaria, Bepotastine 20 mg/day was more effective than placebo in improving levels of itching and eruption, and as effective as terfenadine 120 mg/day with regard to the final global improvement rating and other endpoints. In a noncomparative trial in patients with pruritus associated with skin diseases, the majority of Bepotastine recipients in the overall population, as well as in the specific skin disease subgroups (eczema/dermatitis, prurigo or pruritus cutaneus), had a final global improvement rating of moderate or greater. Bepotastine was generally well tolerated in adult and paediatric patients with allergic conditions.
Bepotastine besilate for the treatment of pruritus
Expert Opin Pharmacother 2013 Dec;14(18):2553-69.PMID:24191914DOI:10.1517/14656566.2013.849242.
Introduction: Bepotastine besilate 1.5% is a newly approved second-generation topical antihistamine indicated for the pruritus associated with allergic conjunctivitis. In Japan, the oral formulation is approved to manage pruritus associated with allergic rhinitis and urticaria. Areas covered: Bepotastine is a piperidine derivative that antagonizes H1 receptors with high selectivity. It has been labeled a dual-acting or multiple-acting antiallergic medication, because it inhibits histamine at H1 receptors and stabilizes mast cells to prevent histamine release. Bepotastine may also have other immunoactive properties, such as inhibition of eosinophil migration, interleukin-5 (IL-5), leukotrienes (e.g., LTB4) and platelet-activating factor (PAF). Human clinical trials demonstrate the efficacy and safety of systemic and ophthalmic Bepotastine for pruritus relief, limited penetration across the blood-brain-barrier and kinetics suitable for twice-daily administration. Expert opinion: Bepotastine besilate 1.5% ophthalmic solution is a safe and effective treatment option for allergic conjunctivitis associated pruritus. Side-effect profile is similar to other ocular antihistamine agents. Additional comparative-effectiveness studies would further advance its clinical use. Oral Bepotastine is a safe and effective treatment option approved in Japan for allergic rhinitis, urticaria and pruritus associated with skin diseases.
Comparative analysis of safety and efficacy of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% in allergic conjunctivitis
Indian J Ophthalmol 2021 Feb;69(2):257-261.PMID:33463568DOI:10.4103/ijo.IJO_2083_20.
Purpose: To compare the efficacy and safety of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2%, and Bepotastine besilate 1.5% ophthalmic solutions in the treatment of allergic conjunctivitis. Methods: This is a prospective, observer-masked, comparative study of 180 patients with mild to moderate allergic conjunctivitis, randomized into three groups of 60 patients each. Each group was assigned to be treated with one of the three treatment options namely Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% ophthalmic solutions. Patients were followed-up at regular intervals with relief and resolution of symptoms and signs noted using Total Ocular Scoring System (TOSS) and hyperaemia scale. Results: All three topical medications were effective in resolving symptoms of the patients with mild to moderate allergic conjunctivitis. Baseline mean TOSS scores for Alcaftadine group, Olopatadine group and Bepotastine besilate group were (7.68±2.32), (7.65±2.32) and (7.45±2.27) respectively as compared to the corresponding TOSS scores on 14th Day (4th visit) which were (0.2 ± 0.43), (0.4 ± 0.56) and (0.1 ± 0.36) respectively. The resolution of symptoms in the Bepotastine and Alcaftadine groups was significantly profound as compared to the Olopatadine group (p = 0.008). Bepotastine and Alcaftadine groups significantly reduced allergic conjunctivitis symptoms compared to Olopatadine group (p = 0.008). Conclusion: All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis. However, Bepotastine and Alcaftadine appear to outweigh Olopatadine in resolving the symptoms of allergic conjunctivitis.
Bepotastine-induced urticaria, cross-reactive with other antihistamines
Asia Pac Allergy 2016 Oct;6(4):253-256.PMID:27803886DOI:10.5415/apallergy.2016.6.4.253.
Second-generation antihistamines are widely prescribed for the control of symptoms of allergic inflammation such as itchy hives, coryza, and itchy eyes. In rare circumstances, these drugs might provoke allergic inflammation. Hypersensitivity to Bepotastine besilate, a second-generation antihistamine has never been reported. A 17-year-old schoolgirl, whose paroxysmal itchy hives had been controlled with Bepotastine, experienced aggravation of the hives. An oral provocation test confirmed her hypersensitivity to Bepotastine and cross-reactivity to levocetirizine. She showed no reaction to chlorpheniramine, ketotifen, or olopatadine among the 13 antihistamines tested. While searching for an antihistamine to control her itchy hives, we found that she also exhibited cross-reactivity to various antihistamines with different chemical structures from that of Bepotastine, which is not predicted according to the chemical classification of antihistamines. We report a case of hypersensitivity to Bepotastine besilate in a patient with chronic spontaneous urticaria.
Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine Bepotastine besilate
Curr Med Res Opin 2010 Oct;26(10):2329-38.PMID:20735291DOI:10.1185/03007995.2010.486753.
Scope: The purpose of this review is to examine published non-clinical literature on the antihistamine Bepotastine besilate, including pharmacokinetic and pharmacologic properties. Methods: Standard literature searches using diverse databases were used to find articles on Bepotastine besilate published between 1997 and 2009. Articles primarily described non-clinical data utilized for the development of an oral formulation of Bepotastine besilate and were published in Japanese. No publications of non-clinical data for an ophthalmic formulation were found in the database searches. Findings: Bepotastine besilate is a second-generation antihistamine drug possessing selective histamine H(1) receptor antagonist activity. Bepotastine has negligible affinity for receptors associated with undesirable adverse effects, including histamine H(3), α(1)-, α(2)-, and β-adrenergic, serotonin (5-HT(2)), muscarinic, and benzodiazepine receptors. Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of LTB(4) and LTD(4) activity. Bepotastine in vivo dose-dependently inhibited the acceleration of histamine-induced vascular permeability and inhibited homologous passive cutaneous anaphylaxis in guinea pig studies. In mouse models of itching, oral Bepotastine inhibited the frequency and duration of scratching behavior. Multiple in vivo animal toxicology studies have demonstrated Bepotastine to be safe with no significant effects on respiratory, circulatory, central nervous, digestive, or urinary systems. The concentration of Bepotastine after intravenous administration of Bepotastine besilate (3 mg/kg) in rats was lower in the brain than in plasma, predicting reduced sedation effects compared to older antihistamines. Conclusion: Non-clinical in vitro and in vivo studies have demonstrated Bepotastine is a histamine H(1) receptor antagonist with favorable pharmacokinetic, pharmacologic, safety, and antihistamine properties as well as operating on other pathways leading to allergic inflammation beyond those directly involving the histamine H(1) receptor.