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氯雷他定

氯雷他定用途

Loratadine(SCH-29851)是H1受体反向激动剂,IC50>32 μM。

氯雷他定名称

[ CAS 号 ]:
79794-75-5

[ 中文名 ]:
氯雷他定

[ 英文名 ]:
Loratadine

[中文别名 ]:

[英文别名 ]:

MFCD00672869
CLARATYNE
Loratadine
Flonidan
Claritine
Loranox
CLARITIN
Tadine
Klaritin
Civeran

氯雷他定生物活性

[ 描述 ]:

Loratadine(SCH-29851)是H1受体反向激动剂,IC50>32 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Kay GG, Harris AG. Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy. 1999 Jul;29 Suppl 3:147-50.

[2]. Menardo JL, Horak F, Danzig MR, Czarlewski W. A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4.

[3]. Monroe EW. Loratadine in the treatment of urticaria. Clin Ther. 1997 Mar-Apr;19(2):232-42.

[4]. Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994 Oct;48(4):617-37.

[5]. Roman IJ, Danzig MR. Loratadine. A review of recent findings in pharmacology, pharmacokinetics, efficacy, and safety, with a look at its use in combination with pseudoephedrine. Clin Rev Allergy. 1993 Spring;11(1):89-110.

[相关活性小分子]

氯雷他定物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
531.3±50.0 °C at 760 mmHg

[ 熔点 ]:
134-136°C

[ 分子式 ]:
C₂₂H₂₃ClN₂O₂

[ 分子量 ]:
382.883

[ 闪点 ]:
275.1±30.1 °C

[ 精确质量 ]:
382.144806

[ PSA ]:
42.43000

[ LogP ]:
5.94

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.614

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable, but may be heat sensitive - refrigerate. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
DMSO: 26 mg/mL, soluble

氯雷他定MSDS

氯雷他定安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ 海关编码 ]:
2933990090

氯雷他定合成路线

氯雷他定上下游产品

氯雷他定上游产品

氯雷他定下游产品

氯雷他定制备

将4-(8-氯-5,6-二氨-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)-1-甲基哌啶溶于甲苯中，滴加氯甲酸乙酯，
反应完毕，加入水，分出苯层，经水洗、干燥、减压浓缩得油状物，用醚浸渍后，经重结晶，即得氯雷他定。

氯雷他定海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

氯雷他定文献

Efficient HPLC method development using structure-based database search, physico-chemical prediction and chromatographic simulation.

J. Pharm. Biomed. Anal. 104 , 49-54, (2014)

Development of a robust HPLC method for pharmaceutical analysis can be very challenging and time-consuming. In our laboratory, we have developed a new workflow leveraging ACD/Labs software tools to im...

Antihistamines modulate the integrin signaling pathway in h9c2 rat cardiomyocytes: Possible association with cardiotoxicity.

Hum. Exp. Toxicol. 34 , 796-807, (2015)

The identification of biomarkers for toxicity prediction is crucial for drug development and safety evaluation. The selective and specific biomarkers for antihistamines-induced cardiotoxicity is not w...

Reliability of computer-assisted method transfer between several column dimensions packed with 1.3-5μm core-shell particles and between various instruments.

J. Pharm. Biomed. Anal. 94 , 188-95, (2014)

In this contribution, the possibility to automatically transfer RPLC methods between different column dimensions and instruments was evaluated using commercial modelling software. The method transfer ...

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