COMPARATIVE AIRWAY AND VASCULAR ACTIVITIES OF LEUKOTRIENE-C-1 AND LEUKOTRIENE-D INVIVO AND INVITRO
COMPARATIVE AIRWAY AND VASCULAR ACTIVITIES OF LEUKOTRIENE-C-1 AND LEUKOTRIENE-D INVIVO AND INVITRO
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DOI：
10.1073/pnas.77.7.4354
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发表时间：
1980-01-01
期刊：
影响因子：
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通讯作者：
COREY, EJ
中科院分区：
文献类型：
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作者：
DRAZEN, JM;AUSTEN, KF;COREY, EJ
本文研究了过敏反应慢反应物质(SRS-A)成分白三烯C-1和D(LTC-1和LTD)对豚鼠肺机械功能、平均体动脉压和皮肤微循环的影响。在体外，LTC-1和LTD都是有效和选择性的外周气道激动剂，比组胺更有活性。LTD在外周呼吸道上的活性浓度是LTC-1的1/100。LTD的量效关系和Fpl 55712[7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxy-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylic酸性单钠盐的拮抗作用与该分子在两种不同的外周呼吸道受体上的活性一致。在体内，LTC-1和LTD对肺力学的影响几乎是相同的，改变的模式与主要作用部位在肺周围是一致的。这两种药物都有直接的全身动脉降压作用，并对皮肤微循环具有血管活性。这些化合物可能是即刻类型超敏反应中病理改变的主要介质，其中外周气道收缩和低血压是显着特征。
The pharmacologic activities of leukotrienes C-1 and D (LTC-1 and LTD), constituents of slow reacting substance of anaphylaxis (SRS-A), were evaluated in vitro on airway contractile tissues and in vivo on pulmonary mechanical function, mean systemic arterial pressure and cutaneous microcirculation in guinea pigs. In vitro both LTC-1 and LTD were potent and selective peripheral airway agonists, being more active than histamine. LTD was active on peripheral airways at concentrations 1/100th those of LTC-1. The concentration-effect relationship for LTD and the profile of antagonism by FPL 55712 [7-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)-2-hydroxy-4-oxo-8-propyl-4H-1-benzopyran-2-carboxylic acid monosodium salt] are consistent with the activity of this molecule at 2 separate peripheral airway receptors. In vivo, LTC-1 and LTD were nearly equally active in their effects on pulmonary mechanics and the pattern of alterations was consistent with the predominant site of action being in the lung periphery. Both agents had a direct systemic arterial hypotensive effect and were vasoactive on the cutaneous microcirculation. The compounds are likely to be major mediators of the pathologic alterations in immediate type hypersensitivity reactions in which peripheral airway constriction and hypotension are prominent features.