Cetirizine: Actions on neurotransmitter receptors

羟嗪 西替利嗪 特非那定 药理学 受体 化学 组胺H1受体 血脑屏障 镇静 中枢神经系统 敌手 医学 内科学 生物化学
作者
Adele M. Snowman,Solomon H. Snyder
出处
期刊:The Journal of Allergy and Clinical Immunology [Elsevier BV]
卷期号:86 (6): 1025-1028 被引量:50
标识
DOI:10.1016/s0091-6749(05)80248-9
摘要

First-generation H 1 -antagonist antihistamines, such as hydroxyzine, have the ability to cross the blood-brain barrier and cause sedation, which limits their usefulness in the treatment of allergic disorders. Cetirizine, a carboxylated metabolite of hydroxyzine, possesses the parent compound's antihistaminic activity but causes less sedation. We compared the activity of cetirizine at central H 1 sites with that of hydroxyzine and terfenadine. We also compared the ability of cetirizine and three antihistamines to cross the blood-brain barrier. In each case we found that the drug's potency at H 1 receptors in the central nervous system was similar to its activity in displacing H 1 receptors in the lung. However, the selectivity for H 1 receptors varied widely from drug to drug. Cetirizine did not bind at any of the receptors investigated, except H 1 sites, even at concentrations as high as 10 μmol/L. Hydroxyzine and dexchlorpheniramine and, to a lesser extent, terfenadine crossed the blood-brain barrier in significant amounts. Cetirizine passed into the central nervous system only half as readily as terfenadine. These findings suggest that cetirizine's low incidence of sedative effects is most likely caused by its diminished potential to cross the blood-brain barrier and also may be partly the result of its greater selectivity for H 1 receptors, compared with its effect at other receptors that may be involved in sedation.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
1秒前
koukousang完成签到,获得积分10
2秒前
乐乐应助张无缺采纳,获得10
3秒前
三三完成签到,获得积分10
3秒前
平常荷花完成签到 ,获得积分10
5秒前
量子星尘发布了新的文献求助10
6秒前
阿胡发布了新的文献求助30
6秒前
水晶李完成签到 ,获得积分10
7秒前
脑洞疼应助静静子采纳,获得100
10秒前
新年好完成签到,获得积分10
11秒前
爆米花应助Michelle采纳,获得10
14秒前
14秒前
LYSM应助晴栀采纳,获得10
15秒前
Bean完成签到,获得积分10
15秒前
15秒前
15秒前
幸福妙柏完成签到 ,获得积分10
16秒前
汕头凯奇完成签到,获得积分10
17秒前
aoba完成签到 ,获得积分10
18秒前
潇洒的平松完成签到,获得积分10
19秒前
qwer完成签到,获得积分10
19秒前
fduqyy发布了新的文献求助10
19秒前
csu_zs完成签到,获得积分10
19秒前
19秒前
LILYpig完成签到 ,获得积分10
20秒前
文静醉易完成签到,获得积分10
20秒前
无聊的翠芙完成签到,获得积分10
21秒前
zhangxuhns完成签到,获得积分10
22秒前
大力哈密瓜完成签到,获得积分10
22秒前
无花果应助碧蓝碧凡采纳,获得10
23秒前
24秒前
25秒前
27秒前
蒋50完成签到,获得积分10
27秒前
不爱喝纯牛奶完成签到,获得积分10
28秒前
28秒前
图图发布了新的文献求助10
28秒前
joysa完成签到,获得积分10
28秒前
风味烤羊腿完成签到,获得积分0
29秒前
29秒前
高分求助中
【提示信息,请勿应助】关于scihub 10000
Les Mantodea de Guyane: Insecta, Polyneoptera [The Mantids of French Guiana] 3000
徐淮辽南地区新元古代叠层石及生物地层 3000
The Mother of All Tableaux: Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 3000
Global Eyelash Assessment scale (GEA) 1000
Picture Books with Same-sex Parented Families: Unintentional Censorship 550
Research on Disturbance Rejection Control Algorithm for Aerial Operation Robots 500
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 4038388
求助须知:如何正确求助?哪些是违规求助? 3576106
关于积分的说明 11374447
捐赠科研通 3305798
什么是DOI,文献DOI怎么找? 1819322
邀请新用户注册赠送积分活动 892672
科研通“疑难数据库(出版商)”最低求助积分说明 815029