20-异亚丙基前列腺素E2（CS-412）的支气管扩张活性

The bronchodilator activity of 20-isopropylidene prostaglandin E2 (CS-412).

作者信息

Yamaguchi T, Sakai K, Yusa T, Yamazaki M

出版信息

Prostaglandins. 1980 Sep;20(3):521-32. doi: 10.1016/0090-6980(80)90040-4.

Abstract

The bronchodilator activity of 20-isopropylidene prostaglandin E2 (CS-412) was studied in vivo. In the conscious guinea pig, aerosols of CS-412, prostaglandin E2 (PGE2), or salbutamol afforded similar protection against histamine-induced convulsions. In the anesthetized guinea pig, where increase in intratracheal pressure was taken as an index of bronchoconstriction, CS-412, PGE2, and salbutamol were equipotent in inhibiting the broncho-constriction induced by histamine. CS-412, PGE2 and salbutamol were equally effective in reducing the serotonin-induced increase in pulmonary resistance in the anesthetized cat. CS-412 was different from PGE2 in bronchoconstrictor activity in anesthetized cats with normal bronchotonus. PGE2 caused bronchoconstriction in the cats. CS-412 showed 30 times less constrictor activity than PGE2. It was concluded that CS-412 is an effective bronchodilator without unfavorable side effects.

摘要

研究了20-异亚丙基前列腺素E2（CS-412）的支气管扩张活性。在清醒的豚鼠中，CS-412、前列腺素E2（PGE2）或沙丁胺醇气雾剂对组胺诱导的惊厥具有相似的保护作用。在麻醉的豚鼠中，以气管内压升高作为支气管收缩的指标，CS-412、PGE2和沙丁胺醇在抑制组胺诱导的支气管收缩方面具有同等效力。CS-412、PGE2和沙丁胺醇在降低麻醉猫中血清素诱导的肺阻力增加方面同样有效。在支气管张力正常的麻醉猫中，CS-412在支气管收缩活性方面与PGE2不同。PGE2可引起猫的支气管收缩。CS-412的收缩活性比PGE2低30倍。得出的结论是，CS-412是一种有效的支气管扩张剂，且无不良副作用。