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Neuronal Signaling
Neuronal Signaling
Histamine Receptor 抑制剂
Fexofenadine HCl
Fexofenadine HCl
目录号 S3208
Fexofenadine HCl抑制组胺H1受体，IC50为246 nM。
10mM (in 1mL DMSO)
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Fexofenadine HCl
结构式分子量:
2015年1月至今，顶级学术期刊发表的应用Selleck产品的部分文献。
质量管理及产品安全说明书
相关化合物库
Fexofenadine HCl
包含在以下化合物库中:
Histamine Receptor产品比较
溶解性(25°C)
Clemastine Fumarate
Latrepirdine
Loratadine
Azelastine HCl
Mianserin HCl
Ranitidine
Bepotastine Besilate
Cetirizine DiHCl
Diphenhydramine HCl
Meclizine 2HCl
Ciproxifan
Mizolastine
Chlorpheniramine Maleate
Desloratadine
Fexofenadine HCl
Nizatidine
Cimetidine
Epinastine HCl
Lafutidine
Tripelennamine HCl
Olopatadine HCl
Buclizine HCl
Brompheniramine hydrogen maleate
Ketotifen Fumarate
Azatadine dimaleate
JNJ-7777120
Hydroxyzine 2HCl
Rupatadine Fumarate
Cyproheptadine HCl
Famotidine
Histamine 2HCl
Levodropropizine
Histamine Phosphate
Doxylamine Succinate
Roxatidine Acetate HCl
Betahistine 2HCl
Pemirolast potassium
Cyclizine 2HCl
Fexofenadine HCl抑制组胺H1受体，IC50为246 nM。
Histamine H1 receptor
Fexofenadine表现出有效且浓度依赖性抗过敏活性，IC50值为95.5nM。Fexofenadine对来自大鼠尾动脉的5-HT2A受体仅表现出弱的竞争性拮抗作用，pA2为5.2。 Caco-2细胞模型中，所有四种P-糖蛋白抑制剂对fexofenadine在两个方向均表现出强的，浓度依赖性作用。Verapamil对P-糖蛋白介导的Fexofenadine的分泌的IC50 为8.44 mM。兔子左心室楔形标本中，Fexofenadine引起QT和Tp-e间隔显著增加，并且在高于其游离TPC 100倍的剂量下达到显著的TdP分数。
Fexofenadine以原形在尿液，胆汁，和胃肠道中排泄，在大鼠体内具有最低的代谢，使其成为研究转运过程的理想探针。在大鼠中，Fexofenadine与Ketoconazole联合给药使Fexofenadine口服接触率增加187%。相反，Fexofenadine与橙汁或苹果汁联合给药使Fexofenadine口服接触率分别减少40%和28%。在小鼠体内， Fexofenadine (17 ml/min/kg)的胆汁排泄清除率占总体清除率(30 ml/min/kg)的60%。基因敲除小鼠的Mdr1a/1b P-gp不影响相对于血浆和肝脏浓度的胆汁排泄清除率，然而P-gp缺乏时，口服给药后会引起血浆浓度增加6倍，和高于3倍的大脑-到-血浆浓度比。
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
用于结合实验的小脑用Ultra-Turrax(设定5，持续20秒)在30体积冰预冷的50mM磷酸缓冲液 (pH 7.5)中均质化，并且以3×105 g离心10分钟(4 ℃)。得到的沉淀重悬浮在30体积冰预冷的50 mM磷酸缓冲液中(pH 7.5)。竞争性试验以一式三份在1 mL终体积中进行。每个试管包含以下物质：0.1 mL不同浓度的置换药物(若不加入竞争性药物，则加入0.1 mL 载体)和包含0.1 mL [3H]-pyrilamine (NEN, 23 Ci/mmol)的缓冲液(终浓度1 nM)。非特异性结合使用10 μM冷的阿司咪唑测定。
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
小鼠大鼠兔豚鼠仓鼠狗
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km 系数36128520
动物A (mg/kg) = 动物B (mg/kg) &&
动物B的Km系数
动物A的Km系数
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
大鼠剂量 (mg/kg) = 小鼠剂量 (22.4 mg/kg) &&
小鼠的Km系数(3)
&= 11.2 mg/kg
大鼠的Km系数(6)
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number
Recruitment
Conditions
Sponsor/Collaborators
Start Date
Active, not recruiting
Drug Interaction
Jules Desmeules|University Hospital, Geneva
November 2014
Drug Interactions
Lexicon Pharmaceuticals
Rhinitis Allergic
Allergic Rhinitis
Indira Gandhi Medical College
April 2014
Not yet recruiting
Uremic Pruritus
National Taiwan University Hospital|Cathay General Hospital
April 2014
C32H39NO4.HCl
3年 -20℃粉状
6个月-80℃溶于溶剂
溶解性 (25°C) *
(198.84 mM)
(198.84 mM)
* &1 mg/ml 指产品微溶或不溶
溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。
Chemical Name
Benzeneacetic acid, 4-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]butyl]-&,&-dimethyl-, hydrochloride (1:1)
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A-438079 HCl
A-438079 HCl 是一种有效的选择性 P2X7 receptor 拮抗剂，pIC50 为 6.9。
Loratadine
Loratadine是一种选择性的histamine H1 receptor拮抗剂，用于治疗过敏。同时还是一种选择性的B(0)AT2抑制剂，其IC50为 4 μM。
JNJ-7777120
JNJ-7777120是第一个，有效的，选择性非咪唑histamine H4 receptor拮抗剂，Ki为4.5 nM，比作用于其他组胺受体选择性高1000倍以上。
Azelastine HCl
Azelastine HCl是有效的，第二代选择性组胺拮抗剂。
Clemastine Fumarate
Clemastine Fumarate是一种选择性组胺H1受体拮抗剂，IC50为3 nM。
Histamine Phosphate
Histamine Phosphate直接作用于血管，扩张H1和H2受体介导的动脉和毛细血管。
Lidocaine是一种选择性的，逆向外周组胺H1受体激动剂，IC50大于32 μM。
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Fexofenadine HCl& allegra (fexofenadine hcl) side effects drug center
Recommended Topic Related To:
"In the largest, most comprehensive, nationwide study to
examine the prevalence of allergies from early childhood to old age, scientists
from the National Institutes of Health report that allergy prevalence is the
same across different regions "...
Allegra Side Effects Center
Medical Editor:
Prescribing Information
For Patients
Last reviewed on RxList
Allegra (fexofenadine hydrochloride) is an antihistamine used to treat allergic symptoms of seasonal allergic rhinitis (sneezing, runny nose, itchy or watery eyes), and urticaria (hives). Allegra is available as a generic drug termed fexofenadine hydrochloride. Allegra is used in adults and children (2 years and older for allergies, 6 months and older for hives) for the control and reduction of the above symptoms. Some common side effects of Allegra include nausea, diarrhea, upset stomach, muscle or back discomfort or pain, sleepiness, headache, and menstrual cramps. Contact your doctor if you have less common side effects of Allegra including allergic reactions, fever, chills, body aches, cough, or other flu symptoms.
Allegra is available in several as tablets in strengths of 30, 60 and 180 mg, as 30 mg fast orally disintegrating tablets (available in foil blister packs and labeled
"ODT"; the drug should not be touched by skin as it may begin to dissolve and reduce the oral dose) and as an oral suspension of 30mg per 5 ml. The dosage is dependent on the age, weight and effec special care should be taken when prescribing this drug to infants and children to make sure the recommended dosage is given. Drugs like ketoconazole and erythromycin may markedly increase the availability of the drug in the body while fruit juices can reduce the concentration. Follow the recommendations of the prescribing doctor to avoid these interactions. There are no studies of Allegra in pregnan the use in the pediatric population is described above. Note that the Allegra ODT tablets (orally disintegrating tablets) contain 5.3 mg of phenylalanine and should not be used by individuals with phenylketonuria.
Our Allegra Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction:
swelling of your face, lips, tongue, or throat.Stop taking fexofenadine and call your doctor if you have fever, chills, body aches, cough, or other flu symptoms.Less serious side effects may include:nausea, diarrhea,drowsiness, ormuscle or back pain.This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Read the entire detailed patient monograph for
Side Effects
Cough, fever, or stomach upset may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
If your doctor has prescribed this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Read the entire patient information overview for
Side Effects (Adverse Reactions)
SIDE EFFECTS
Clinical Studies Experience
are conducted under widely varying conditions,
rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The safety data described below reflect exposure to ALLEGRA (fexofenadine hydrochloride) in 5083 patients in trials for
and chronic idiopathic urticaria.
In these trials, 3010 patients 12 years of age and older with seasonal allergic rhinitis were exposed to ALLEGRA (fexofenadine hydrochloride) at doses of 20 to 240 mg twice daily or 120 to 180 mg once daily.
A total of 646 patients 6 to 11 years of age with seasonal allergic rhinitis were exposed to ALLEGRA (fexofenadine hydrochloride) at doses of 15 to 60 mg twice daily. The duration of treatment in these trials was 2 weeks. A total of 534 patients 6 months to 5 years of age with allergic rhinitis were exposed to ALLEGRA (fexofenadine hydrochloride) at doses of 15 to 30 mg twice daily. The duration of treatment in these trials ranged from 1 day to 2 weeks.
There were 893 patients 12 years of age and older with chronic idiopathic urticaria exposed to ALLEGRA (fexofenadine hydrochloride) at doses of 20 to 240 mg
twice daily or 180 mg once daily.
The duration of treatment in these trials was 4 weeks.
Seasonal Allergic Rhinitis
Adults and Adolescents: In
seasonal allergic
rhinitis clinical trials in subjects 12 years of age and older, 2439 subjects
received ALLEGRA (fexofenadine hydrochloride) capsules at doses of 20 mg to 240 mg twice
daily. All adverse reactions that were reported by greater than 1% of subjects
who received the recommended daily dose of ALLEGRA (fexofenadine hydrochloride) (60 mg
capsules twice daily) are listed in Table 1.
In another placebo-controlled clinical study in the United States, 571 subjects aged 12 years and older received ALLEGRA (fexofenadine hydrochloride) tablets at doses of 120 or 180 mg once daily. Table 1 also lists adverse reactions that were reported by greater than 2% of subjects treated with ALLEGRA (fexofenadine hydrochloride) tablets at doses of 180 mg once daily.
of adverse reactions, including somnolence/fatigue, was not dose-related and was similar across subgroups defined by age, gender, and race.
Table 1: Adverse reactions in subjects aged 12 years and
older reported in placebo-controlled seasonal allergic rhinitis clinical trials
in the United States
Twice-daily dosing with fexofenadine capsules at rates of
greater than 1%
Adverse reaction
Fexofenadine 60 mg Twice Daily
Placebo Twice Daily
Dysmenorrhea
Once-daily dosing with ALLEGRA (fexofenadine hydrochloride) tablets
at rates of greater than 2%
Adverse reaction
Fexofenadine 180 mg Once Daily
The frequency and magnitude of laboratory abnormalities were similar in ALLEGRA (fexofenadine hydrochloride)- and placebo-treated subjects.
Pediatrics: Table 2 lists adverse reactions in subjects aged
6 years to 11 years of age which were reported by greater than 2% of subjects
treated with ALLEGRA (fexofenadine hydrochloride) tablets at a dose of 30 mg twice daily
in placebo-controlled seasonal allergic rhinitis studies in the United States
and Canada.
Table 2: Adverse reactions reported in placebo-controlled
seasonal allergic rhinitis studies in pediatric subjects aged 6 years to 11
years in the United States and Canada at rates of greater than 2%
Adverse reaction
Fexofenadine 30 mg Twice Daily
Upper Respiratory Tract Infection
Otitis Media
Table 3 lists adverse reactions in subjects 6 months to 5 years of age which were reported by greater than 2% of subjects treated with ALLEGRA (fexofenadine hydrochloride) in 3 open single- and multiple-dose pharmacokinetic studies and 3 placebo-controlled safety studies with ALLEGRA (fexofenadine hydrochloride) capsule content (484 subjects) and suspension (50 subjects) at doses of 15 mg (108 subjects) and 30 mg (426 subjects) given twice a day.
Table 3: Adverse reactions reported in placebo-controlled
studies in pediatric subjects with allergic rhinitis aged 6 months to 5 years
of age at rates greater than 2%
Adverse reaction
Fexofenadine 15 mg Twice Daily
Fexofenadine 30 mg Twice Daily
Fexofenadine Total
Twice Daily
Somnolence/Fatigue
Rhinorrhea
Chronic Idiopathic Urticaria
Adverse reactions reported by subjects 12 years of age and older in placebo-controlled
chronic idiopathic urticaria studies were similar to those reported in placebo-controlled
seasonal allergic rhinitis studies.
In placebo-controlled chronic idiopathic urticaria clinical trials, 726 subjects
12 years of age and older received ALLEGRA (fexofenadine hydrochloride) tablets at doses
of 20 to 240 mg twice daily. Table 4 lists adverse reactions in subjects aged
12 years and older which were reported by greater than 2% of subjects treated
with ALLEGRA (fexofenadine hydrochloride) 60 mg tablets twice daily in controlled clinical
studies in the United States and Canada.
In a placebo-controlled clinical study in the United States, 167 subjects aged 12 years and
older received ALLEGRA (fexofenadine hydrochloride) 180 mg tablets. Table 4 also lists adverse reactions that were reported by greater than 2% of subjects treated with ALLEGRA (fexofenadine hydrochloride) tablets at doses of 180 mg once daily.
Table 4: Adverse reactions reported in subjects 12 years
of age and older in placebo-controlled chronic idiopathic urticaria studies
Twice-daily dosing with ALLEGRA (fexofenadine hydrochloride) in studies
in the UnitedStates and Canada at rates of greater than 2%
Adverse reaction
Fexofenadine 60 mg Twice Daily
Stomach discomfort
Pain in extremity
Once-daily dosing with ALLEGRA (fexofenadine hydrochloride) in a study
in the United States at rates of greater than 2%
Adverse reaction
Fexofenadine 180 mg Once Daily
The safety of ALLEGRA (fexofenadine hydrochloride) in the treatment of chronic idiopathic
urticaria in pediatric patients 6 months to 11 years of age is based on the
safety profile of ALLEGRA (fexofenadine hydrochloride) in adults and pediatric patients
at doses equal to or higher than the recommended dose [see ].
Postmarketing Experience
In addition to the adverse reactions reported during clinical studies and listed above, the following adverse events have been identified during post-approval use of ALLEGRA (fexofenadine hcl).
Because these events are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Events that have been reported rarely during postmarketing experience include: , nervousness,
or paroniria, and hypersensitivity reactions (including , urticaria, , chest tightness, , flushing, , and ).
Read the entire FDA prescribing information for
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