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一种11-脱氧前列腺素(AY 23 578)的支气管扩张活性。

The bronchodilator acitivity of an 11-deoxyprostaglandin (AY 23 578).

作者信息

Greenberg R, Smorong K

出版信息

Can J Physiol Pharmacol. 1975 Oct;53(5):799-809. doi: 10.1139/y75-110.

Abstract

The bronchodilator activity of AY-23 578 was studied in vivo and in vitro techniques. In the conscious guinea pig, aerosols of AY-23 578, prostaglandin (PGE2) E2, and isoproterenol afforded significant protection against histamine-induced convulsions. In the anesthetized guinea pig, where changes in tracheal pressure were taken as an index of bronchoconstriction, AY-23 578, PGE2, and isoproterenol were equipotent in inhibiting the bronchoconstriction induced by histamine. AY-23 578, PGE2, and isoproterenol reduced or prevented neostigmine-, prostaglandin F2alpha- or carbachol-induced increases in pulmonary resistance, and decreases in dynamic compliance in the anesthetized cat. The activities of the former two compounds were qualitatively similar but less potent than isoproterenol. In both the guinea pig and the cat, the aerosol administration of effective bronchodilator doses of AY-23 578 did not exhibit any significant cardiovascular effects. Both AY-23 578 and PGE2 caused relaxation of the isolated guinea pig tracheal strip; PGE2 was about six times more potent than AY-23 578. It is concluded that AY-23 578 is an effective bronchodilator in both the guinea pig and cat.

摘要

采用体内和体外技术研究了AY - 23 578的支气管扩张活性。在清醒的豚鼠中,AY - 23 578、前列腺素(PGE2)E2和气雾剂异丙肾上腺素对组胺诱导的惊厥有显著的保护作用。在麻醉的豚鼠中,以气管压力变化作为支气管收缩的指标,AY - 23 578、PGE2和异丙肾上腺素在抑制组胺诱导的支气管收缩方面具有同等效力。AY - 23 578、PGE2和异丙肾上腺素可降低或预防新斯的明、前列腺素F2α或卡巴胆碱诱导的麻醉猫肺阻力增加和动态顺应性降低。前两种化合物的活性在性质上相似,但效力低于异丙肾上腺素。在豚鼠和猫中,气雾吸入有效支气管扩张剂量的AY - 23 578均未表现出任何显著的心血管效应。AY - 23 578和PGE2均可使离体豚鼠气管条松弛;PGE2的效力约为AY - 23 578的六倍。结论是AY - 23 578在豚鼠和猫中都是一种有效的支气管扩张剂。

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