Fexofenadine HCl
(Synonyms: 盐酸非索非那定; MDL-16455 hydrochloride; Terfenadine carboxylate hydrochloride) 目录号 : GC10966
Fexofenadine HCl是一种具有口服活性和非镇静作用的组胺H1受体拮抗剂。
Cas No.:153439-40-8
Sample solution is provided at 25 µL, 10mM.
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Fexofenadine HCl is an orally active and nonsedative histamine H1 receptor antagonist[1]. Histamine H1 receptor is a G protein coupled receptor (GPCR) widely expressed in airway, vascular smooth muscle and central nervous system(CNS) that, upon histamine binding, mediates classic type-I hypersensitivity reactions including allergic inflammation, increased vascular permeability and pruritus[2]. Fexofenadine HCl can be used in researches of allergic rhinitis and chronic idiopathic urticarial research via antagonism of the histamine H1 receptor[3][4].
In vitro, pretreatment of nasal fibroblast with 1, 10, or 100μM Fexofenadine HCl for 1 hour before histamine stimulation significantly inhibited the expression of IL-6 protein in a dose dependent manner and actively suppressed pp38 and NF-κB expression but not pERK and pJNK[5]. Pretreatment of cultured human monocytes with Fexofenadine HCl (0.1mM or 1mM; 20h) significantly inhibits the production of LTC4, LTD4, and LTE4 stimulated by zymosan, as well as the production of PGE2 stimulated by lipopolysaccharide[6].
In vivo, Fexofenadine HCl (5-20mg/kg/day; p.o.; 3 weeks) inhibited eosinophilia and systemic allergic responses in C57BL/6 mice infected with T. spiralis[1]. Fexofenadine HCl (2.5mg per dose; twice daily; p.o.; 6 days) treatment of sensitized mice prevented airway hyperresponsiveness in both primary sensitization and challenge, as well as in adoptive transfer experiments, and was accompanied with decreased bronchoalveolar lavage and tissue eosinophilia, lymphocyte numbers, and TH2 cytokine production[7].
References:
[1] Watanabe N, Matsuda E, Masuda A, Nariai K, Shibasaki T. The effects of fexofenadine on eosinophilia and systemic anaphylaxis in mice infected with Trichinella spiralis. Int Immunopharmacol. 2004;4(3):367-375.
[2] Smit MJ, Hoffmann M, Timmerman H, Leurs R. Molecular properties and signalling pathways of the histamine H1 receptor. Clin Exp Allergy. 1999;29 Suppl 3:19-28.
[3] Ming X, Knight BM, Thakker DR. Vectorial transport of fexofenadine across Caco-2 cells: involvement of apical uptake and basolateral efflux transporters. Mol Pharm. 2011;8(5):1677-1686.
[4] Markham A, Wagstaff AJ. Fexofenadine. Drugs. 1998;55(2):269-276.
[5] Park IH, Um JY, Cho JS, Lee SH, Lee SH, Lee HM. Histamine Promotes the Release of Interleukin-6 via the H1R/p38 and NF-κB Pathways in Nasal Fibroblasts. Allergy Asthma Immunol Res. 2014;6(6):567-572.
[6] Juergens UR, Darlath W, Stober M, et al. Differential effects of fexofenadine on arachidonic acid metabolism in cultured human monocytes. Pharmacology. 2006;76(1):40-45.
[7] Gelfand EW, Cui ZH, Takeda K, Kanehiro A, Joetham A. Fexofenadine modulates T-cell function, preventing allergen-induced airway inflammation and hyperresponsiveness. J Allergy Clin Immunol. 2002;110(1):85-95.
Fexofenadine HCl是一种具有口服活性和非镇静作用的组胺H1受体拮抗剂[1]。组胺H1受体是一种G蛋白偶联受体（GPCR），广泛分布于呼吸道、血管平滑肌和中枢神经系统，当与组胺结合时，可介导包括过敏性炎症、血管通透性增加和瘙痒在内的经典 I 型超敏反应[2]。Fexofenadine HCl通过拮抗组胺H1受体，可用于过敏性鼻炎和慢性特发性荨麻疹的研究[3][4]。
体外实验中，用1、10或100µM的Fexofenadine HCl预处理鼻成纤维细胞1小时，可以剂量依赖方式显著抑制组胺刺激后IL-6蛋白的表达，并抑制p38磷酸化和NF-κB的表达，但对pERK和pJNK无影响[5]。此外，用0.1mM或1mM的Fexofenadine HCl预处理培养的人单核细胞20小时，可显著抑制由酵母聚糖刺激产生的LTC4、LTD4和LTE4，以及由脂多糖刺激产生的PGE2[6]。
体内实验中，Fexofenadine HCl (5-20mg/kg/天; 口服给药；连续3周) 可抑制感染T. spiralis的C57BL/6 小鼠中的嗜酸性粒细胞增多症和全身过敏反应[1]。对致敏小鼠进行Fexofenadine HCl（2.5mg/次；每天两次；灌胃给药; 持续6天）处理，可在初始致敏和激发以及过继性转移实验中预防气道高反应性，并降低支气管肺泡灌洗液和组织中嗜酸性粒细胞、淋巴细胞数量以及TH2型细胞因子产生[7]。
| Cell experiment [1]: | |
Cell lines | Nasal fibroblasts |
Preparation Method | Nasal fibroblasts were isolated from surgical tissues by enzymatic digestion with collagenase (500U/mL), hyaluronidase (30U/mL), and DNase (10U/mL). Cells were cultured in Dulbecco’s Modified Eagle’s Medium containing 10% (v/v) heat-inactivated fetal bovine serum, 1% (v/v), 10,000U/mL penicillin, and 10,000μg/mL streptomycin. Cells were pretreated with 1, 10, or 100μM Fexofenadine HCl for 1 hour and then stimulated with histamine (100μM) for 24 hours. |
Reaction Conditions | 1, 10, or 100μM; 1h |
Applications | Fexofenadine HCl inhibited the expression of IL-6 protein in a dose dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c mice |
Preparation Method | Female BALB/c mice 10 to 12 weeks of age were sensitized by means of intraperitoneal injection of 20µg of OVA emulsified in 2.25mg of aluminum hydroxide in a total volume of 100µL on days 1 and 14. Mice were challenged for 20 minutes through the airways daily with OVA (1% in saline) for 3 days (days 26, 27, and 28) by using ultrasonic nebulization. The drug Fexofenadine HCl was suspended in saline and administered by means of gavage (without anesthesia) at a dose of 2.5mg twice daily beginning 3 days before allergen challenge and on each of the days of allergen challenge. Airway responsiveness was assessed with a single-chamber, whole-body plethysmograph. |
Dosage form | 2.5mg twice daily; p.o.; 6days |
Applications | Fexofenadine HCl treatment of sensitized mice prevented airway hyperresponsiveness. |
References: | |
| Cas No. | 153439-40-8 | SDF | |
| 别名 | 盐酸非索非那定; MDL-16455 hydrochloride; Terfenadine carboxylate hydrochloride | ||
| 化学名 | 2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid;hydrochloride | ||
| Canonical SMILES | CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O.Cl | ||
| 分子式 | C32H39NO4.HCl | 分子量 | 538.12 |
| 溶解度 | ≥ 26.9mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8583 mL | 9.2916 mL | 18.5832 mL |
| 5 mM | 0.3717 mL | 1.8583 mL | 3.7166 mL |
| 10 mM | 0.1858 mL | 0.9292 mL | 1.8583 mL |
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