(R)-Cetirizine (hydrochloride)
(Synonyms: 盐酸左西替利嗪,(R)-Cetirizine dihydrochloride) 目录号 : GC41715
A selective histamine H1 receptor antagonist
Cas No.:130018-87-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(R)-Cetirizine is the (R)-enantiomer of the histamine H1 receptor antagonist and second generation antihistamine cetirizine . (R)-Cetirizine binds to the H1 receptor with higher affinity than cetirizine (Kis = 3 and 6 nM, respectively) and is 25,000-100,000-fold selective for H1 receptors over muscarinic M1-M5 receptors. It decreases production of RANTES and eotaxin following antigen stimulation in mouse eosinophils in vitro in a concentration-dependent manner with a minimum effective concentration (MEC) of 0.05 µM. Intranasal administration of (R)-cetirizine (0.01-1%) dose-dependently decreases histamine-induced nasal rubbing and sneezing in mice. Formulations containing (R)-cetirizine have been used in the treatment of allergic rhinitis and chronic idiopathic urticaria.
| Cas No. | 130018-87-0 | SDF | |
| 别名 | 盐酸左西替利嗪,(R)-Cetirizine dihydrochloride | ||
| Canonical SMILES | ClC1=CC=C([C@H](N2CCN(CCOCC(O)=O)CC2)C3=CC=CC=C3)C=C1.Cl.Cl | ||
| 分子式 | C21H25ClN2O3•2HCl | 分子量 | 461.8 |
| 溶解度 | DMF: 3 mg/ml,DMSO: 12 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1654 mL | 10.8272 mL | 21.6544 mL |
| 5 mM | 0.4331 mL | 2.1654 mL | 4.3309 mL |
| 10 mM | 0.2165 mL | 1.0827 mL | 2.1654 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Improved transdermal delivery of cetirizine hydrochloride using polymeric microneedles
Daru 2019 Dec;27(2):673-681.PMID:31630328DOI:10.1007/s40199-019-00301-3.
Purpose: The aim of this study was to design and characterize microneedle patch formulation containing cetirizine hydrochloride. Methods: Chitosan was co-formulated with cetirizine hydrochloride. Transdermal patches were prepared by casting this solution to microneedle molds. Control patches were formulated by casting this solution to a plain cuvet of same area as mold but lacking microneedles. An array of methods namely; differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and scanning electron microscopy (SEM) were employed for the characterization of the films and the microneedles accordingly whereas in vitro permeation studies were conducted across rat skin. Light microscopy was performed to assess any histological changes upon microneedles application onto the rat skin. Results: The patches had a reproducible thickness (0.86 ± 0.06 mm) and folding endurance. Both the blank and drug loaded patches had 100 microneedles each of 300 micrometre length. In addition, the microneedle patches were ascribed with a two-fold increase in drug permeation across rat skin in the presence of microneedles as compared to the control formulations. Histological examination confirms a minimal invasion of the skin conferred by the microneedles. Conclusion: The microneedle patches serve as an alternate route of drug administration in patients with nausea and swelling difficulties. Graphical abstract Microneedle patch manifest a two-fold increase in the skin permeation of Cetirizine hydrochloride as compared to the control that is drug loaded patch without microneedles.
New Electrochemical Sensor Based on Hierarchical Carbon Nanofibers with NiCo Nanoparticles and Its Application for Cetirizine hydrochloride Determination
Materials (Basel) 2022 May 20;15(10):3648.PMID:35629673DOI:10.3390/ma15103648.
A new electrochemical sensor based on hierarchical carbon nanofibers with Ni and Co nanoparticles (eCNF/CNT/NiCo-GCE) was developed. The presented sensor may be characterized by high sensitivity, good electrical conductivity, and electrocatalytic properties. Reproducibility of its preparation expressed as %RSD (relative standard deviation) was equal to 9.7% (n = 5). The repeatability of the signal register on eCNF/CNT/NiCo-GCE was equal to 3.4% (n = 9). The developed sensor was applied in the determination of the antihistamine drug-cetirizine hydrochloride (CTZ). Measurement conditions, such as DPV (differential pulse voltammetry) parameters, supporting electrolyte composition and concentration were optimized. CTZ exhibits a linear response in three concentration ranges: 0.05-6 µM (r = 0.988); 7-32 (r = 0.992); and 42-112 (r = 0.999). Based on the calibration performed, the limit of detection (LOD) and limit of quantification (LOQ) were calculated and were equal to 14 nM and 42 nM, respectively. The applicability of the optimized method for the determination of CTZ was proven by analysis of its concentration in real samples, such as pharmaceutical products and body fluids (urine and plasma). The results were satisfactory and the calculated recoveries (97-115%) suggest that the method may be considered accurate. The obtained results proved that the developed sensor and optimized method may be used in routine laboratory practice.
Enantioseparation of cetirizine by chromatographic methods and discrimination by 1H-NMR
Drug Test Anal 2009 Mar;1(3):118-24.PMID:20355184DOI:10.1002/dta.23.
Cetirizine is an antihistaminic drug used to prevent and treat allergic conditions. It is currently marketed as a racemate. The H1-antagonist activity of cetirizine is primarily due to (R)-levocetirizine. This has led to the introduction of (R)-levocetirizine into clinical practice, and the chiral switching is expected to be more selective and safer. The present work represents three methods for the analysis and chiral discrimination of cetirizine. The first method was based on the enantioseparation of cetirizine on silica gel TLC plates using different chiral selectors as mobile phase additives. The mobile phase enabling successful resolution was acetonitrile-water 17: 3, (v/v) containing 1 mM of chiral selector, namely hydroxypropyl-beta-cyclodextrin, chondroitin sulphate or vancomycin hydrochloride. The second method was a validated high performance liquid chromatography (HPLC), based on stereoselective separation of cetirizine and quantitative determination of its eutomer (R)-levocetirizine on a monolithic C18 column using hydroxypropyl-beta-cyclodextrin as a chiral mobile phase additive. The resolved peaks of (R)-levocetirizine and (S)-dextrocetirizine were confirmed by further mass spectrometry. The third method used a (1)H-NMR technique to characterize cetirizine and (R)-levocetirizine. These methods are selective and accurate, and can be easily applied for chiral discrimination and determination of cetirizine in drug substance and drug product in quality control laboratory. Moreover, chiral purity testing of (R)-levocetirizine can also be monitored by the chromatographic methods.
Recent environmental applications of and development prospects for immobilized laccase: a review
Biotechnol Genet Eng Rev 2020 Oct;36(2):81-131.PMID:33435852DOI:10.1080/02648725.2020.1864187.
Laccases have enormous potential as promising 'green' biocatalysts in environmental applications including wastewater treatment and polluted soil bioremediation. The catalytic oxidation reaction they perform uses only molecular oxygen without other cofactors, and the only product after the reaction is water. The immobilization of laccase offers several improvements such as protected activity and enhanced stability over free laccase. In addition, the reusability of immobilized laccase is adistinct advantage for future applications. This review covers the sources of and progress in laccase research, and discusses the different methodologies of laccase immobilization that have emerged in the recent 5-10 years, as well as its applications to environmental fields, and evaluates these emerging technologies. Abbreviations: (2,4,6-TCP): 2,4,6-trichlorophenol; (2,4-DCP): 2,4-dichlorophenol; (ABTS), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid); (ACE), acetaminophen; (BC-AS), almond shell; (BC-PM), pig manure; (BC-PW), pine wood; (BPA), bisphenol A; (BPA), bisphenol A; (BPF), bisphenol F; (BPS), bisphenol S; (C60), fullerene; (Ca-AIL), calcium-alginate immobilized laccase; (CBZ), carbamazepine; (CETY), cetirizine; (CHT-PGMA-PEI-Cu (II) NPs), Cu (II)-chelated chitosan nanoparticles; (CLEAs), cross-linked enzyme aggregates; (CMMC), carbon-based mesoporous magnetic composites; (COD), chemical oxygen demand; (CPH), ciprofloxacin hydrochloride; (CS), chitosan; (CTC), chlortetracycline; (Cu-AIL), copper-alginate immobilized laccase; (DBR K-4BL), Drimarene brilliant red K-4BL; (DCF), diclofenac; (E1),estrone; (E2), 17 β-estradiol; (EDC), 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride; (EDCs), endocrine disrupting chemicals; (EE2), 17α-ethinylestradiol; (EFMs), electrospun fibrous membranes; (FL), free laccase; (fsMP), fumed silica microparticles; (GA-CBs), GLU-crosslinked chitosan beads; (GA-CBs), glutaraldehyde-crosslinked chitosan beads; (GA-Zr-MOF), graphene aerogel-zirconium-metal organic framework; (GLU), glutaraldehyde; (GO), graphene oxide; (HMCs), hollow mesoporous carbon spheres; (HPEI/PES), hyperbranched polyethyleneimine/polyether sulfone; (IC), indigo carmine; (IL), immobilized laccase; (kcat), catalytic constant; (Km), Michealis constant; (M-CLEAs), Magnetic cross-linked enzyme aggregates; (MMSNPs-CPTS-IDA-Cu2+), Cu2+-chelated magnetic mesoporous silica nanoparticles; (MSS), magnetic mesoporous silica spheres; (MWNTs), multi-walled carbon nanotubes; (MWNTs), multi-walled carbon nanotubes; (NHS), N-hydroxy succinimide; (O-MWNTs), oxidized-MWNTs; (P(AAm-NIPA)), poly(acrylamide-N-isopropylacrylamide); (p(GMA)), poly(glycidyl methacrylate); (p(HEMA)), poly(hydroxyethyl methacrylate); (p(HEMA-g-GMA)-NH2, poly(glycidyl methacrylate) brush grafted poly(hydroxyethyl methacrylate); (PA6/CHIT), polyamide 6/chitosan; (PAC), powdered active carbon; (PAHs), polycyclic aromatic hydrocarbons; (PAM-CTS), chitosan grafted polyacrylamide hydrogel; (PAN/MMT/GO), polyacrylonitrile/montmorillonite/graphene oxide; (PAN/PVdF), polyacrylonitrile/polyvinylidene fluoride; (PEG), poly ethylene glycol; (PEI), Poly(ethyleneimine); (poly(4-VP)), poly(4-vinyl pyridine); (poly(GMA-MAA)), poly(glycidyl methacrylate-methacrylic acid); (PVA), polyvinyl alcohol; (RBBR), Remazol Brilliant Blue R; (SDE), simulated dye effluent; (semi-IPNs), semi-interpenetrating polymer networks; (TC), tetracycline; (TCH), tetracycline hydrochloride; (TCS), triclosan; (Vmax), maximum activity; (Zr-MOF, MMU), micro-mesoporous Zr-metal organic framework.
Dose dependency of brain histamine H(1) receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [11C]doxepin
Hum Psychopharmacol 2009 Oct;24(7):540-8.PMID:19697300DOI:10.1002/hup.1051.
Aims: The strength of sedation due to antihistamines can be evaluated using positron emission tomography (PET). The purpose of the present study is to measure histamine H(1) receptor (H(1)R) occupancy following oral administration of cetirizine (10 and 20 mg) in order to examine dose dependency. Methods: Fifteen healthy male volunteers (age range, 20-35 years) were divided into 3 subgroups and were studied following single oral administration of cetirizine at 10 mg (n = 5) and 20 mg (n = 5) or hydroxyzine at 30 mg (n = 5) using PET with 11C-doxepin. Each subject was scanned also following the administration of placebo. Binding potential and H(1)RO values were calculated in the prefrontal and anterior cingulate cortices. Subjective sleepiness was also measured, and the correlation to H(1)RO was examined for each antihistamine. Results: The averaged H(1)ROs of cetirizine 10 mg, 20 mg, and hydroxyzine 30 mg in the prefrontal and cingulate cortices was 12.6%, 25.2%, and 67.6%, respectively. The H(1)RO of hydroxyzine 30 mg correlated well with subjective sleepiness (p < 0.001); however, those of cetirizine 10 and 20 mg showed no correlation with subjective sleepiness. Conclusion: It was demonstrated that the brain penetration of orally administered cetirizine was dose-dependent. Cetirizine 10 mg, with its low H(1)RO and thus minimal sedation, could be more safely used than cetirizine 20 mg for the treatment of various allergic disorders.