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中氮茚并三唑衍生物在血液、心血管和呼吸系统中的药理学

Pharmacology of mesoionic oxatriazole derivatives in blood, cardiovascular and respiratory systems.

作者信息

Corell T, Pedersen S B, Lissau B, Moilanen E, Metsä-Ketelä T, Kankaanranta H, Vuorinen P, Vapaatalo H, Rydell E, Andersson R

机构信息

A/S GEA Farmaceutisk Fabrik, Pharmacological and Toxicological Department Hvidovre, Denmark.

出版信息

Pol J Pharmacol. 1994 Nov-Dec;46(6):553-66.

PMID:7542520
Abstract

Mesoionic oxatriazole derivatives were synthetized by GEA LTD1. The GEA compounds (GEAC) constitute a new class of NO-donors, some of which stimulate selectively guanylate cyclase abiding either platelets or leukocytes or lung tissues. In consequence, some of GEAC are potent anti-platelet, fibrinolytic, thrombolytic or broncholytic agents, both in vitro and in vivo. GEAC synergize with prostacyclin in their thrombolytic actions. They also suppress the release of histamine and leukotriene B4, and prevent degranulation of granulocytes. Methylene blue reduces, and zaprinast augments their pharmacological effects. It is suggested that within a series of the newly synthetized GEA compounds there are likely to be found potential candidates for treating either thrombotic or asthmatic disorders.

摘要

GEA有限公司合成了中氮茚并三唑衍生物。GEA化合物(GEAC)构成了一类新型的一氧化氮供体,其中一些能选择性地刺激鸟苷酸环化酶,作用于血小板、白细胞或肺组织。因此,一些GEAC在体外和体内都是有效的抗血小板、纤维蛋白溶解、溶栓或支气管溶解剂。GEAC在溶栓作用中与前列环素协同作用。它们还能抑制组胺和白三烯B4的释放,并防止粒细胞脱颗粒。亚甲蓝会降低其药理作用,而扎普司特会增强其药理作用。有人认为,在一系列新合成的GEA化合物中,可能会找到治疗血栓形成或哮喘疾病的潜在候选药物。

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