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二盐酸匹卡司特(奥洛他定),一种新型的抗过敏介质释放及作用抑制剂。

Picumast dihydrochloride (Auteral), a new anti-allergic inhibitor of mediator release and action.

作者信息

Wilhelms O H, Roesch A, Schaumann W

机构信息

Medical Research, Boehringer Mannheim GmbH, Mannheim, FRG.

出版信息

Agents Actions Suppl. 1991;34:335-49.

PMID:1686528
Abstract

Picumast dihydrochloride (PDH), (3,4-dimethyl-7-[4-chlorobenzyl) piperazine-1-yl]propoxycoumarin dihydrochloride) is a prophylactically active anti-allergic compound which combines inhibition of mediator release and action. The activity profile of PDH differs clearly from that of known prophylactic anti-allergic drugs such as DSCG and ketotifen. Other inhibitory actions of PDH in addition to its H1-antagonism (and that of its metabolites M2 and M1) may be the cause of the suppression of immediate and late phase allergic reactions in animals as well as allergic rhinitis and bronchial responsiveness and symptom scores in asthmatic patients.

摘要

盐酸匹卡司特(PDH),即(3,4-二甲基-7-[4-氯苄基)哌嗪-1-基]丙氧基香豆素二盐酸盐),是一种具有预防活性的抗过敏化合物,兼具抑制介质释放和作用的特性。PDH的活性特征与已知的预防性抗过敏药物如色甘酸钠和酮替芬明显不同。除了其H1拮抗作用(及其代谢产物M2和M1的H1拮抗作用)外,PDH的其他抑制作用可能是其抑制动物速发和迟发性过敏反应以及哮喘患者过敏性鼻炎、支气管反应性和症状评分的原因。

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