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11-脱氧-11α,12α-甲撑前列腺素E2,一种强效短效支气管扩张剂。

11-Deoxy-11 alpha,12 alpha-methanoprostaglandin E2, a potent, short-acting bronchodilator.

作者信息

Davis R, Garay G L, Guzman A, Muchowski J M, Rooks W H, Tomolonis A J, Velarde E

出版信息

J Pharm Sci. 1986 Mar;75(3):307-12. doi: 10.1002/jps.2600750322.

Abstract

11-Deoxy-11 alpha,12 alpha-methanoprostaglandin E2 (1b) and the corresponding methyl ester 7a were highly potent, but short acting, bronchodilators both by the intravenous (80 and 10 times PGE2, respectively) and aerosol (2 and approximately 1 times PGE2) routes, as measured by the Konzett-Rössler assay. The 11 beta,12 beta-methano compound 15a was two orders of magnitude less active than 7a. In rhesus monkeys anesthetized by aerosol administration, 1b was 10-50% as potent as, and had a duration of action similar to, PGE1 in the inhibition of methacholine-induced increases in airway resistance. At doses effective in preventing the methacholine response, 1b increased the heart rate (less than or equal to 30%) and precipitated mild upper airway irritation.

摘要

通过Konzett-Rössler测定法测量,11-脱氧-11α,12α-甲撑前列腺素E2(1b)及其相应的甲酯7a都是强效但作用时间短的支气管扩张剂,静脉注射(分别为PGE2的80倍和10倍)和气雾剂给药(分别为PGE2的2倍和约1倍)时均如此。11β,12β-甲撑化合物15a的活性比7a低两个数量级。在通过气雾剂给药麻醉的恒河猴中,在抑制乙酰甲胆碱诱导的气道阻力增加方面,1b的效力为PGE1的10%-50%,且作用持续时间与PGE1相似。在有效预防乙酰甲胆碱反应的剂量下,1b会使心率增加(≤30%),并引发轻度上呼吸道刺激。

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