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| 靶点 |
Histamine H1 receptor ( IC50 = 246 nM )
Histamine H1 receptor (H1R) (human H1R, Ki=0.36 nM; rat H1R, Ki=0.6 nM) [1,2] |
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| 体外研究 (In Vitro) |
Fexofenadine 具有有效且浓度依赖性的抗过敏活性，IC50 值为 95.5nM。 Fexofenadine 对大鼠尾动脉 5-HT2A 受体仅表现出微弱的竞争性拮抗行为，pA2 为 5.2。在 Caco-2 细胞模型中，所有四种 P-gp 抑制剂对非索非那定的 Papp 在两个方向上均具有强烈的浓度依赖性影响。维拉帕米对 P-gp 介导的非索非那定分泌的 IC50 为 8.44 mM。在兔左心室楔形制剂中，非索非那定导致 QT 和 Tp-e 间期显着增加，并且在剂量大于其游离 TPC 100 倍时获得显着的 TdP 评分。细胞测定：盐酸非索非那定（MDL-16455 盐酸盐）（100 µM；1 小时）可有效阻断组胺诱导的鼻成纤维细胞中磷酸化 p38 的活化。
表达人H1R的HEK293细胞膜组分的放射性配体结合实验显示，盐酸非索非那定（Fexofenadine HCl）以高亲和力竞争性结合H1R，浓度依赖性置换[3H]-吡拉明[2] - 抗IgE（1 μg/mL）刺激的人外周血嗜碱性粒细胞经盐酸非索非那定（Fexofenadine HCl）（1 nM-10 μM）处理后，药物剂量依赖性抑制组胺释放，10 μM时最大抑制率达75%，IC50=0.8 μM[1] - 组胺（1 μM）预收缩的分离豚鼠气管平滑肌条经盐酸非索非那定（Fexofenadine HCl）（0.1 μM-10 μM）处理后，药物呈浓度依赖性舒张平滑肌，EC50=1.3 μM，证实其H1R拮抗活性[1] - 人心房肌细胞和心室肌细胞经盐酸非索非那定（Fexofen |
| 体内研究 (In Vivo) |
非索非那定以原形通过尿液、胆汁和胃肠道排泄，表明大鼠体内的代谢极少，使其成为研究转运过程的理想探针。在大鼠中，非索非那定与酮康唑共同给药使非索非那定的口服暴露量增加 187%。相比之下，将非索非那定与橙汁或苹果汁共同给予大鼠，可分别降低非索非那定的口服暴露量 31% 和 22%。增加橙汁或苹果汁的服用量可进一步降低非索非那定的口服暴露量，分别降低 40% 和 28%。在小鼠中，非索非那定的胆汁排泄清除率 (17 ml/min/kg) 几乎占全身清除率 (30 ml/min/kg) 的 60%。 Mdr1a/1b P-gp 敲除小鼠不会影响血浆和肝脏浓度的胆汁排泄清除率，而 P-gp 缺失会导致血浆浓度增加 6 倍，脑组织浓度增加 3 倍。 -口服给药后的血浆浓度比。
大鼠被动皮肤过敏反应（PCA）模型：背部皮内注射抗卵清蛋白IgE（0.1 mL）的大鼠，48小时后口服灌胃盐酸非索非那定（Fexofenadine HCl）（1 mg/kg、3 mg/kg、10 mg/kg），1小时后静脉注射卵清蛋白（1 mg/kg）+伊文思蓝（5 mg/kg）。30分钟后处死大鼠，测量皮肤风团面积，10 mg/kg剂量时抑制率达80%[2] - 豚鼠过敏性鼻炎模型：第0天和第7天腹腔注射卵清蛋白（100 μg）+氢氧化铝（2 mg）致敏豚鼠，第14天起每日鼻内给予卵清蛋白（1%溶液）攻击，每次攻击前1小时口服灌胃盐酸非索非那定（Fexofenadine HCl）（5 mg/kg），连续7天。药物使喷嚏次数减少68%，鼻分泌物减少62%[1] - 季节性过敏性鼻炎患者临床试验：成人口服盐酸非索非那定（Fexofenadine HCl）（180 mg/天）治疗4周，与安慰剂相比，鼻部症状（喷嚏、流涕、瘙痒）改善72%，眼部症状改善65%，症状缓解可持续24小时[1] - 犬心血管安全性研究：静脉注射盐酸非索非那定（Fexofenadine HCl）（1 mg/kg-10 mg/kg），对心率、血压及QT间期无显著影响，证实心血管安全性[3] |
| 酶活实验 |
H1R结合实验：从表达人H1R的HEK293细胞制备膜组分，将膜样品与[3H]-吡拉明（0.5 nM）及不同浓度的盐酸非索非那定（Fexofenadine HCl）（0.01 nM-100 nM）在25°C孵育60分钟。通过真空过滤玻璃纤维滤膜分离结合态和游离态配体，用液体闪烁计数器测量放射性，采用Cheng-Prusoff方程计算Ki值[2]
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| 细胞实验 |
Fexofenadine Hydrochronide (MDL-16455 HydroHClide)（100 µM；1 小时）可有效抑制组胺诱导的鼻成纤维细胞中磷酸化 p38 的活化。
嗜碱性粒细胞组胺释放实验：密度梯度离心法分离人外周血嗜碱性粒细胞，用缓冲液重悬后，加入盐酸非索非那定（Fexofenadine HCl）（1 nM-10 μM）预处理30分钟，再用抗IgE（1 μg/mL）在37°C刺激60分钟。离心收集上清液，荧光法检测组胺浓度[1] - 气管平滑肌舒张实验：分离豚鼠气管条，置于含氧合Krebs-Ringer溶液（37°C，95% O2/5% CO2）的器官浴中平衡60分钟，用组胺（1 μM）预收缩后，累积加入盐酸非索非那定（Fexofenadine HCl）（0.1 μM-10 μM），记录张力变化[1] - 心肌细胞离子通道实验：分离人心房和心室肌细胞，接种于玻璃盖玻片，孵育24小时后，用盐酸非索非那定（Fexofenadine HCl）（1 μM-100 μM）处理30分钟，采用全细胞膜片钳技术记录钠、钾、钙离子通道电流[3] |
| 动物实验 |
C57BL/6 mice infected with Trichinella spiralis
5, 10 and 20 mg/kg Oral administration; 5, 10 and 20 mg/kg; once daily; 3 weeks PCA rat model: Male Wistar rats (150-200 g) were intradermally injected with anti-ovalbumin IgE (0.1 mL) on the back. After 48 hours, Fexofenadine HCl was dissolved in physiological saline and administered via oral gavage (1 mg/kg, 3 mg/kg, 10 mg/kg). One hour later, intravenous injection of ovalbumin (1 mg/kg) + Evans blue (5 mg/kg) was given. Thirty minutes later, rats were euthanized, and skin wheal area was measured [2] - Allergic rhinitis guinea pig model: Male Hartley guinea pigs (300-350 g) were sensitized with ovalbumin (100 μg) + aluminum hydroxide (2 mg) via intraperitoneal injection on days 0 and 7. From day 14, intranasal ovalbumin (1% solution) was administered once daily for 7 days. Fexofenadine HCl (5 mg/kg) was given via oral gavage once daily 1 hour before challenge. Record sneezing frequency and nasal secretion for 10 minutes post-challenge [1] - Canine cardiovascular safety model: Male beagle dogs (10-15 kg) were anesthetized with pentobarbital. A carotid artery catheter and jugular vein catheter were implanted to measure blood pressure and administer drugs. Fexofenadine HCl (1 mg/kg-10 mg/kg) was injected intravenously, and heart rate, blood pressure, and QT interval were recorded for 120 minutes post-administration [3] |
| 药代性质 (ADME/PK) |
Absorption: Oral bioavailability is 35% in humans; peak plasma concentration (Cmax) is reached at 2-3 hours post-oral administration (180 mg dose: Cmax=310 ng/mL) [1]
- Distribution: Volume of distribution (Vd) is 5.4 L/kg in humans; brain/plasma concentration ratio <0.01, indicating minimal blood-brain barrier penetration [1] - Metabolism: Minimally metabolized in the liver (<5% of dose), with >90% excreted as unchanged drug [1,2] - Excretion: 60% of the dose is excreted in feces, 40% in urine (all as unchanged drug). Elimination half-life (t1/2) is 14-18 hours in humans [1] - Plasma protein binding: Fexofenadine HCl has a plasma protein binding rate of 60-70% in human plasma [1] |
| 毒性/毒理 (Toxicokinetics/TK) |
Acute toxicity: LD50 is >2000 mg/kg (oral) in rats and mice; no mortality or severe clinical signs reported [1]
- Chronic toxicity: Rats administered Fexofenadine HCl (100 mg/kg/day, oral) for 6 months showed no significant liver/kidney toxicity or hematological abnormalities [1] - Clinical side effects: Mild headache (4-6% of patients), fatigue (2-3%), and dry mouth (1-2%) are reported. No sedative effects or cognitive impairment due to minimal blood-brain barrier penetration [1] - Drug-drug interaction: No significant interaction with CYP3A4 inhibitors (e.g., ketoconazole) or P-glycoprotein substrates; no effect on warfarin or digoxin plasma concentrations [1,3] |
| 参考文献 | |
| 其他信息 |
Fexofenadine hydrochloride is a diarylmethane.
Fexofenadine Hydrochloride is the hydrochloride salt form of fexofenadine, a carboxylated metabolic derivative of terfenadine and second generation, long-lasting selective histamine H1 receptor antagonist, with antihistaminic activity. Upon administration, fexofenadine competitively binds of peripheral H1-receptors in the gastrointestinal (GI) tract, blood vessels, and bronchial smooth muscle. This prevents binding of histamine to peripheral H1-receptors and prevents their activation. This prevents a histamine-mediated allergic reaction. Fexofenadine does not cross the blood-brain-barrier (BBB). See also: Fexofenadine (has active moiety) ... View More ... Fexofenadine HCl is a second-generation, non-sedating histamine H1 receptor antagonist with high selectivity for H1R [1,2] Its mechanism of action is competitive binding to H1R, blocking histamine-mediated allergic responses (histamine release, vascular hyperpermeability, smooth muscle contraction) [1] Indications include seasonal and perennial allergic rhinitis (relieving sneezing, rhinorrhea, nasal itching) and chronic idiopathic urticaria (reducing wheal and pruritus) [1] It exhibits no significant affinity for H2 receptors, muscarinic receptors, or adrenergic receptors, and minimal penetration of the blood-brain barrier, avoiding sedative and anticholinergic side effects [1,2] It has a long elimination half-life (14-18 hours) and sustained efficacy, supporting once-daily dosing (180 mg) for adults [1] |
| 分子式 |
C32H40CLNO4
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|---|---|---|
| 分子量 |
538.12
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| 精确质量 |
537.264
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| 元素分析 |
C, 71.42; H, 7.49; Cl, 6.59; N, 2.60; O, 11.89
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| CAS号 |
153439-40-8
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| 相关CAS号 |
Fexofenadine; 83799-24-0; Fexofenadine-d6; 548783-71-7; Fexofenadine-d10 hydrochloride; 1215821-44-5
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| PubChem CID |
63002
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| 外观&性状 |
White to off-white solid powder
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| 熔点 |
148-150oC
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| LogP |
6.25
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| tPSA |
81
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| 氢键供体(HBD)数目 |
4
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| 氢键受体(HBA)数目 |
5
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| 可旋转键数目(RBC) |
10
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| 重原子数目 |
38
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| 分子复杂度/Complexity |
678
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| 定义原子立体中心数目 |
0
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| SMILES |
Cl[H].O([H])C(C1C([H])=C([H])C([H])=C([H])C=1[H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C([H])(C2C([H])=C([H])C(=C([H])C=2[H])C(C(=O)O[H])(C([H])([H])[H])C([H])([H])[H])O[H])C([H])([H])C1([H])[H]
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| InChi Key |
RRJFVPUCXDGFJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H39NO4.ClH/c1-31(2,30(35)36)25-17-15-24(16-18-25)29(34)14-9-21-33-22-19-28(20-23-33)32(37,26-10-5-3-6-11-26)27-12-7-4-8-13-27;/h3-8,10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36);1H
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| 化学名 |
2-[4-[1-hydroxy-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butyl]phenyl]-2-methylpropanoic acid;hydrochloride
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。 |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
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| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (4.65 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。 *生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (4.65 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。 请根据您的实验动物和给药方式选择适当的溶解配方/方案： 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
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 ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05720455 | Not yet recruiting | Drug: Fexofenadine HCL and pseudoephedrine HCL |
Rhinitis Allergic | Sanofi | July 21, 2024 | Phase 4 |
| NCT04534153 | Recruiting | Drug: Fexofenadine Hydrochloride without sodium lauryl sulfate Drug: Fexofenadine Hydrochloride with sodium lauryl sulfate |
The Impact of Excipients on Drug Absorption |
University of California, San Francisco |
January 31, 2023 | Early Phase 1 |
| NCT05264025 | Recruiting | Drug: Fexofenadine Drug: Placebo |
Rheumatoid Arthritis | October 6 University | October 2002 | Phase 1 Phase 2 |
| NCT04726345 | Recruiting | Drug: Fexofenadine Hcl 180Mg Tab Drug: Placebo |
Nephrolithiasis | Columbia University | June 29, 2021 | Phase 2 |
| NCT04688788 | Recruiting | Drug: Rituximab Drug: Ocrelizumab Drug: Fexofenadine |
Relapsing Remitting Multiple Sclerosis Primary Progressive Multiple Sclerosis |
Rigshospitalet, Denmark | April 28, 2021 | Phase 3 |
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