四种13,14-二脱氢-PGE2类似物的体内和体外支气管扩张活性。

Bronchodilator activity in vivo and in vitro of four 13,14-didehydro-PGE2 analogues.

作者信息

Ceserani R, Marotta F, Usardi M M, Orlando N, Gandolfi C, Bianco S

出版信息

Prostaglandins Med. 1979 Jun;2(6):459-66. doi: 10.1016/0161-4630(79)90131-9.

PMID:552097

Abstract

The bronchodilator activity of four analogues of PGE2: 13,14-didehydro-PGE2 (I), 20-methyl-13,14-didehydro-PGE2 (II), 16 S-methyl-13,14-didehydro-PGE2 (III) and 16 R-methyl-13,14-didehydro-PGE2 (IV) was studied in vivo and in vitro. The potency of III and IV when administered by aerosol to conscious guinea pigs was four times that of PGE2 in protecting against histamine-induced convulsion; I and II were less active. Compound III administered by aerosol to anaesthetized guinea pigs was six times more potent than PGE2 in protecting against i.v. histamine-induced increase of intractracheal pressure and the effect was longer-lasting. All the compounds caused relaxation of carbachol-induced tone in isolated guinea pig tracheal strips.

摘要

研究了前列腺素E2（PGE2）的四种类似物：13,14-二脱氢-PGE2（I）、20-甲基-13,14-二脱氢-PGE2（II）、16S-甲基-13,14-二脱氢-PGE2（III）和16R-甲基-13,14-二脱氢-PGE2（IV）的支气管扩张活性。在体内和体外实验中，将III和IV通过气雾剂给予清醒豚鼠时，其预防组胺诱发惊厥的效力是PGE2的四倍；I和II的活性较低。将化合物III通过气雾剂给予麻醉豚鼠时，其预防静脉注射组胺引起的气管内压升高的效力比PGE2高六倍，且作用更持久。所有化合物均可使离体豚鼠气管条中卡巴胆碱诱导的张力松弛。