基本信息

技术规格

物性(参考值)

相关法规

基本信息

产品描述

Desloratadine是一种有效的人组胺H1受体拮抗剂，IC50为51nM.

靶点（IC50 & Targe）

H1 receptor,51nM

体外研究

Desloratadine是卡巴胆碱诱导的离体兔虹膜平滑肌收缩的竞争性拮抗剂，pA2为6.67。[1] Desloratadine与人H1受体结合，在氚标记的美吡拉敏中，Ki值为0.87 nM。Desloratadine (100 nM到10 μM)抑制IgE介导的和非IgE介导的人嗜碱粒细胞中细胞因子IL-4 和IL-13的产生。Desloratadine (300 nM到100 μM)抑制IgE介导的和非IgE介导的组胺从人周边血液嗜碱性粒细胞的释放。在从过敏性鼻炎或过敏性哮喘患者体内取得的嗜酸细胞中，Desloratadine (0.1 μM到10 μM)能够抑制血小板激活因子诱导的嗜伊红性趋药性和TNF-α诱导的嗜酸性细胞粘附。[2] Desloratadine (1 μM-10 μM)剂量依赖性抑制组胺和LTC4从人嗜碱粒细胞中释放。Desloratadine (0.1 μM-10 μM)剂量依赖性抑制嗜碱粒细胞中IL-13分泌。Desloratadine (10 μM)预处理导致培养的嗜碱粒细胞中诱导的细胞因子大量减少。在培养的嗜碱粒细胞中，Desloratadine (10 μM)预处理引起IL-4信子与抗IgE激活减少大约80%。Desloratadine (10 μM)也会抑制组胺和IL-4蛋白质分泌到培养的嗜碱粒细胞的上层清夜中。[3] [3H] Desloratadine与在CHO细胞中表达的人组胺H1受体结合，Kd为1.1 nM。在竞争性结合研究中，Desloratadine比cetirizine，ebastine，fexofenadine，和loratadine分别有效52，57，194，以及153倍。[4]

体内研究

Desloratadine (1 毫克/毫升，3 毫克/毫升和10 毫克/毫升)引起豚鼠体内剂量依赖性和持久性瞳孔放大。[1] Desloratadine抑制小鼠体内组胺诱导的足肿胀，ED50为0.15 毫克/千克。Desloratadine抑制豚鼠体内组胺侵袭上呼吸道引起的血管通透性增加，ED50为0.9 微克。[2] Desloratadine (5 毫克/千克)通过破坏有意识小鼠体内的血脑屏障而抑制氧化震颤素诱导的肿瘤。Desloratadine (1.0毫克/千克)显著抑制毁脑脊髓大鼠体内氧化震颤素诱导的(0.00125毫克/千克，0.0025 毫克/千克，和0.02 毫克/千克) dP/dt减少，由剂量-响应曲线右移指示。[5]

动物实验

Animal Models: 雄性豚鼠

Formulation: 20% 聚乙二醇-300

Dosages: 10毫克/千克

Administration: 皮下注射

(Only for Reference)

参考文献

[1] Cardelús I, et al. Eur J Pharmacol, 1999, 374(2), 249-25

[2] Geha RS, et al. J Allergy Clin Immunol, 2001, 107(4), 751-762.

[3] Schroeder JT, et al. Clin Exp Allergy, 2001, 31(9), 1369-1377.

[4] Anthes JC, et al. Eur J Pharmacol, 2002, 449(3), 229-237.

[5] Howell G 3rd, et al. BMC Pharmacol, 2005, 5, 13.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P391 P501
UN号码	3077
危险分类	9
包装等级	III
WGK	3
RTECS	DE8011000

基本信息

Ref#
46292

分子式
C19H19ClN2

分子量
236.64

产品说明

一般描述

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.
Desloratadine is one of the orally active, highly selective peripheral H₁ receptor antagonists that does not exert any significant effect on the central and autonomic nervous systems. The potency of desloratadine is more than that of loratadine and it exhibits substantial overall pharmacological profile.

应用

These Secondary Standards are qualified as Certified Reference Materials. These are suitable for use in several analytical applications including but not limited to pharma release testing, pharma method development for qualitative and quantitative analyses, food and beverage quality control testing, and other calibration requirements.
Desloratadine may be used as a pharmaceutical reference standard for the determination of the analyte in pharmaceutical formulations and plasma samples by various chromatography techniques.

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

分析说明

These secondary standards offer multi-traceability to the USP, EP and BP primary standards, where they are available.

其他说明

This Certified Reference Material (CRM) is produced and certified in accordance with ISO 17034 and ISO/IEC 17025. All information regarding the use of this CRM can be found on the certificate of analysis.

附注

To see an example of a Certificate of Analysis for this material enter LRAC2775 in the Documents slot below. This is an example certificate only and may not be the lot that you receive.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

产品说明

应用

Desloratadine has been used to test its effect on embryoid body development in in vitro gastrulation model of P19C5 stem cells. It has also been used as an antihistamine mimic in rats and to treat lung cancer (A549) and glioblastoma (U87) cells in various cellular studies.

包装

10, 50 mg in glass bottle

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

其他说明

Tandem Mass Spectrometry data independently generated by Scripps Center for Metabolomics is available to view or download in PDF. D1069.pdf Tested metabolites are featured on Scripps Center for Metabolomics METLIN Metabolite Database. To learn more, visit sigma.com/metlin.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

包装

Unit quantity: 100 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

包装

Unit quantity: 5 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.
For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

Sales restrictions may apply.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

Desloratadine is a selective and nonsedating histamine H1 receptor antagonist, an active metabolite of loratadine (Claritin), used to relieve hay fever and allergy symptoms with less drowsiness than other antihistamines; does not significantly inhibits cardiac K+ channels at clinically achievable blood levels. Free from antimuscarinic/anticholinergic effects.

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.  ​

其他说明

USP issued SDS can be found here.
Sales restrictions may apply.

法律信息

Clarinex is a registered trademark of Schering Corp.

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .