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]。