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地氯雷他定

地氯雷他定用途

Desloratadine(Sch34117)是人H1受体拮抗剂。

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地氯雷他定名称

[ CAS 号 ]:
100643-71-8

[ 中文名 ]:
地氯雷他定

[ 英文名 ]:
Desloratadine

[中文别名 ]:

[英文别名 ]:

UNII-FVF865388R
AzoMyr
DESLORATIDINE
MFCD00871949
Opulis
Desloratadine
Allex
Descarboethoxyoratidine
Neoclarityn
Aerius

地氯雷他定生物活性

[ 描述 ]:

Desloratadine(Sch34117)是人H1受体拮抗剂。

[ 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]. Geha, R.S. and E.O. Meltzer, Desloratadine: A new, nonsedating, oral antihistamine. J Allergy Clin Immunol, 2001. 107(4): p. 751-62.

[2]. Schroeder, J.T., et al., Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Clin Exp Allergy, 2001. 31(9): p. 1369-77.

[3]. Anthes, J.C., et al., Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol, 2002. 449(3): p. 229-37.

[相关活性小分子]

地氯雷他定物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
467.9±45.0 °C at 760 mmHg

[ 熔点 ]:
150-151°C

[ 分子式 ]:
C₁₉H₁₉ClN₂

[ 分子量 ]:
310.821

[ 闪点 ]:
236.8±28.7 °C

[ 精确质量 ]:
310.123688

[ PSA ]:
24.92000

[ LogP ]:
6.77

[ 外观性状 ]:
米色固体

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.626

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
水溶性：微溶；易溶于：乙醇

地氯雷他定MSDS

地氯雷他定安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R11:Highly Flammable.

[ 安全声明 (欧洲) ]:
S16-S23-S36/37/39

[ 危险品运输编码 ]:
1993

地氯雷他定合成路线

地氯雷他定上下游产品

地氯雷他定上游产品

地氯雷他定下游产品

地氯雷他定制备

将氯雷他定加到含氢氧化钠的乙醇溶液中,回流反应.产物经冰乙酸、氯仿提取等处理得地氯雷他定乙酸盐。将其溶于水中,用稀碳酸钾溶液碱化,用氯仿提取.提取液水洗,浓缩,加入己烷浸渍,经重结晶,得地氯雷他定.

1. 氯雷他定[4-(8-氯-5,6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)-1-哌啶羧酸乙酯]的制备

在反应瓶中加入8-氯-6,11-二氢-11-(1-甲基-4-哌啶叉)-5H-苯并[5,6]-环庚并[1,2-b]吡啶45.g(0.141mol)和甲苯320ml,搅拌溶解,于约80 ºC左右慢慢加入氯甲酸乙酯45.9g(40.4ml,0.423mol),保温在80ºC搅拌反应1h.TLC跟踪,反应毕冷至环境温度,减压蒸除过量的氯甲酸乙酯,剩余物加水450ml和甲苯适量,在60ºC下继续搅拌1h.用NaOH水溶液调至pH10,静置分层,分出有机相,水相再用甲苯提取,合并有机相,无水Na2SO4干燥,过滤,滤液减压浓缩,剩余物溶于乙腈中,用活性炭脱色,热过滤,滤液浓缩至结晶浆状物出现,冷至5ºC,结晶全部析出,过滤,干燥得白色固体氯雷他定[4-(8-氯-5,6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)-1-哌啶羧酸乙酯]42.2g,收率78.2%,mp134.5~136ºC,Rf0.51[展开剂:浓氨水/甲醇(1.5:100)]

2. 8-氯-6,11-二氢-11-(4-亚哌啶基)-5H-苯并[5,6]环庚并[1,2-b]吡啶(地洛他定)的合成

在反应瓶中加入乙醇305ml、KOH 150g(2.68mol)和氯雷他定[4-(8-氯-5,6-二氢-11H-苯并[5,6]环庚并[1,2-b]吡啶-11-亚基)-1-哌啶羧酸乙酯]39g(0.101mol),在N2保护下搅拌回流反应5~6h.当析出大量固体时即为反应终点$冷却后移至蒸馏装置减压浓缩回收乙醇,剩余物用盐水稀释,用乙酸乙酯提取3次$有机层合并,用水洗,无水Na2SO4干燥,过滤,滤液蒸除溶剂,得到固体8-氯-6,11-二氢-11-(4-亚哌啶基)-5H-苯并[5,6]环庚并[1,2-b]吡啶(地洛他定)粗品24.5g,收率77%,为白色固体,mp154~155 ºC.将粗品用甲基异丁基酮(MIBK)245ml控温在70~80 ºC溶解,若未全溶则补加MIBK适量,冷却加活性炭12.6g,保温搅拌(80ºC)20~30min.热过滤,滤液冷却析晶,过滤,干燥得8-氯-6,11-二氢-11-(4-亚哌啶基)-5H-苯并[5,6]环庚并[1,2-b]吡啶(地洛他定)纯品22.3g,精制收率91%,mp156.5~157.0 ºC.

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地氯雷他定文献

Utility of cerebrospinal fluid drug concentration as a surrogate for unbound brain concentration in nonhuman primates.

Drug Metab. Pharmacokinet. 29(5) , 419-26, (2014)

In central nervous system drug discovery, cerebrospinal fluid (CSF) drug concentration (C(CSF)) has been widely used as a surrogate for unbound brain concentrations (C(u,brain)). However, previous rod...

A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement.

Drug Metab. Dispos. 43(4) , 523-33, (2015)

Desloratadine (Clarinex), the major active metabolite of loratadine (Claritin), is a nonsedating long-lasting antihistamine that is widely used for the treatment of allergic rhinitis and chronic idiop...

Differential thermodynamic driving force of first- and second-generation antihistamines to determine their binding affinity for human H1 receptors.

Biochem. Pharmacol. 91(2) , 231-41, (2014)

Differential binding sites for first- and second-generation antihistamines were indicated on the basis of the crystal structure of human histamine H1 receptors. In this study, we evaluated differences...

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2019-01-13 17:57:27

导读：地氯雷他定是氯雷他定的主要活性代谢物，属于第三代抗组胺药物。商品名芙必叮，是目前我国批准上市的第一个第三代抗组胺药，其药理作用与氯雷他定相似，但作用更强，副作用更少。具有长效抗组胺作用，但不会阻滞心脏钾通道，从而改善药物对心血管系统的安全性。最大特点是无镇静作用、无心脏毒性。主要用于缓解过敏...