Bepotastine
(Synonyms: 贝他斯汀) 目录号 : GC39479
Bepotastine是一种非镇静的、具有口服活性的第二代组胺H1受体（histamine H1 receptor）拮抗剂，其作用选择性高于H3受体、α1、α2和β肾上腺素能受体、多巴胺D2受体、血清素5-HT2受体、乙酰胆碱迷走神经受体以及苯二氮䓬受体。
Cas No.:125602-71-3
Sample solution is provided at 25 µL, 10mM.
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Bepotastine is a non-sedating, orally active second-generation histamine H1 receptor antagonist with higher selectivity than H3 receptors, α1, α2 and β adrenergic receptors, dopamine D2 receptors, serotonin 5-HT2 receptors, vagus nerve acetylcholine receptors, and benzodiazepine receptors [1]. Bepotastine can inhibit the upregulation of histamine-mediated nerve growth factor (NGF) expression [2]. Bepotastine can be used in studies of allergic rhinitis, allergic conjunctivitis, and urticaria/pruritus [3-4].
In vitro, Bepotastine (10, 100, and 1000μM; 120min) pretreatment reduced histamine release from glomerular mesangial cells (RPMCs) induced by ionizing agent A23187, and could dose-dependently inhibit the chemotaxis of eosinophils induced by leukotriene B4 (LTB4) [5]. Bepotastine (50μM; 1h) treatment significantly reduced the mRNA expression of nerve growth factor (NGF) in human epidermal keratinocytes (NHEKs) mediated by histamine [6].
In vivo, treatment with Bepotastine (10μL 1% (w/v) eye drop) 20, 40 and 60 minutes before platelet-activating factor (PAF) stimulation was able to significantly inhibit the eosinophil infiltration in the conjunctiva of guinea pigs with PAF-induced allergic conjunctivitis model [5]. Bepotastine (3 and 10mg/kg/day; single dose) oral treatment 1 hour later could effectively inhibit scratching behavior induced by histamine in mice, and significantly reduced the serum LTB4 levels in the NC/Nga dermatitis model mice at a dose of 10mg/kg/day [7].
References:
[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] Tamura T, Amano T, Ohmori K, et al. The effects of olopatadine hydrochloride on the number of scratching induced by repeated application of oxazolone in mice[J]. European journal of pharmacology, 2005, 524(1-3): 149-154.
[3] Khilnani G, Khilnani A K, Thaddanee R. Learning pharmacology by metaphors: A tale of antihistamines[J]. National Journal of Physiology, Pharmacy and Pharmacology, 2020, 10(8): 693-693.
[4] Sil A, Rahaman S, Mondal N, et al. An investigator-blind randomized controlled trial comparing effectiveness, safety of levocetirizine and bepotastine in chronic urticaria[J]. Indian Journal of Dermatology, 2021, 66(5): 472-478.
[5] Kida T, Fujii A, Sakai O, et al. Bepotastine besilate, a highly selective histamine H(1) receptor antagonist, suppresses vascular hyperpermeability and eosinophil recruitment in in vitro and in vivo experimental allergic conjunctivitis models. Exp Eye Res. 2010;91(1):85-91.
[6] Kamata Y, Sakaguchi A, Umehara Y, et al. Bepotastine besilate downregulates the expression of nerve elongation factors in normal human epidermal keratinocytes. J Dermatol Sci. Published online April 23, 2018. [7] Tanizaki H, Kambe N, Nakamura Y, Tanaka A, Matsuda H, Miyachi Y. Oral administration of bepotastine besilate suppressed scratching behavior of atopic dermatitis model NC/Nga mice. Int Arch Allergy Immunol. 2008;145(4):277-282.
Bepotastine是一种非镇静的、具有口服活性的第二代组胺H1受体（histamine H1 receptor）拮抗剂，其作用选择性高于H3受体、α1、α2和β肾上腺素能受体、多巴胺D2受体、血清素5-HT2受体、乙酰胆碱迷走神经受体以及苯二氮䓬受体 [1]。Bepotastine可抑制组胺介导的神经生长因子（NGF）表达上调 [2]。Bepotastine可用于过敏性鼻炎，过敏性结膜炎和荨麻疹/瘙痒症的研究 [3-4]。
在体外，Bepotastine（10、100和1000μM; 120min）预处理减少了电离质A23187诱导的肾小球系膜细胞（RPMCs）的组胺释放，并能够剂量依赖性地抑制白三烯B4（LTB4）诱导的嗜酸性粒细胞的趋化性 [5]。Bepotastine（50μM; 1h）处理显著降低了组胺介导的人类表皮角质形成细胞(NHEKs）中神经生长因子（NGF）的mRNA表达 [6]。
在体内，在血小板活化因子（PAF）刺激前20、40和60分钟通过Bepotastine（10μL 1%（w/v）滴眼液）治疗能够显著抑制PAF诱导的过敏性结膜炎模型豚鼠的结膜嗜酸性粒细胞浸润 [5]。Bepotastine（3和10mg/kg/day; single dose）口服治疗后1小时能够有效抑制组胺诱发的小鼠抓挠行为，并在10mg/kg/day剂量下显著降低NC/Nga皮炎模型小鼠的血清LTB4水平 [7]。
| Cell experiment [1]: | |
Cell lines | Renal glomerular mesangial cells (RPMCs) |
Preparation Method | For the assay of histamine release, 1mL of RPMC suspension (2 × 104 cells/mL) was mixed with 1mL of Tyrode’s solution containing 0.2% ethanol with or without Bepotastine at final concentrations of 10, 100, or 1000μM, and the mixture was pre-incubated for 120min at 37°C in a humidified atmosphere (5% CO2). After preincubation, 10μL of the calcium ionophore A23187 in dimethylsulfoxide was added to each well to make a final concentration of 0.01μM A23187 and the plates were incubated for 10min. The plates were then placed on ice to terminate the reaction and each cell suspension was centrifuged at 200×g for 8min at 4°C. The supernatant was collected to determine the amount of histamine release from RPMCs. Histamine in the precipitant was determined by adding Tyrode’s solution and homogenizing by sonication. The sonicated samples were centrifuged at 800×g for 10min at 4°C and the supernatant was collected to determine the amount of residual histamine. |
Reaction Conditions | 10, 100 and 1000μM; 120min |
Applications | Bepotastine pretreatment reduced the histamine release from RPMCs induced by the A23187. |
| Animal experiment [1]: | |
Animal models | Guinea pigs (allergic conjunctivitis models) |
Preparation Method | Guinea pigs (6-week-old) topically received 10μL of Bepotastine eye drops (1.0% (w/v)) in one eye 3 times at intervals of 20min. At 20min after the last instillation of Bepotastine, 10μL of platelet-activating factor (PAF) dissolved in saline at a final concentration of 0.1% (w/v) was topically applied into their conjunctiva to induce eosinophil infiltration. Six hours after PAF instillation, the animals were euthanized and each conjunctiva was removed for determination of eosinophil peroxidase (EPO) activity. |
Dosage form | 1.0% (w/v) for 10µL; Eye drop; 3 times at intervals of 20min (in one eye) |
Applications | Treatment with Bepotastine was able to significantly inhibit the PAF-induced eosinophil infiltration in the guinea pig conjunctiva. |
References: | |
| 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 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL |
| 5 mM | 514.3 μL | 2.5714 mL | 5.1428 mL |
| 10 mM | 257.1 μL | 1.2857 mL | 2.5714 mL |
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