Tomioka K, Terai M, Maeno H
Arch Int Pharmacodyn Ther. 1977 Apr;226(2):224-34.
The bronchodilator activity of synthetic 16(S)-methyl-20-methoxy-PGE2 (YPG-209) was investigated in guinea-pigs. The potency of YPG-209 in relaxing the isolated trachea contracted by histamine was 10 times smaller than that of PGE2, and was not reduced by propranolol, while in the anesthetized animals YPG-209 given by an intravenous route was 230 times as potent in inhibiting an increase in the airway resistance induced by histamine as PGE2. When administered either intraduodenally to the anesthetized animals or orally to the conscious ones, YPG-209 showed a pronounced protection against histamine-induced bronchoconstriction, in contrast to PGE2 which had no significant protecting effect. Neither hypotension nor diarrhea could be observed at the doses of YPG-209 exhibiting a considerable bronchodilator effect. The hydroxyl group at carbon-15 of YPG-209 was little oxidized by 15-hydroxy prostaglandin dehydrogenase which was purified from the lung of guinea-pigs, consistent with the comparably long lasting bronchodilator activity of YPG-209 in vivo.
在豚鼠中研究了合成的16(S)-甲基-20-甲氧基-PGE2（YPG-209）的支气管扩张活性。YPG-209舒张由组胺收缩的离体气管的效力比PGE2小10倍，且不受普萘洛尔影响，而在麻醉动物中，静脉注射YPG-209抑制组胺诱导的气道阻力增加的效力是PGE2的230倍。当对麻醉动物十二指肠内给药或对清醒动物口服给药时，YPG-209对组胺诱导的支气管收缩有显著的保护作用，而PGE2则无明显保护作用。在呈现出相当大支气管扩张作用的YPG-209剂量下，未观察到低血压或腹泻。YPG-209的C-15位羟基很少被从豚鼠肺中纯化的15-羟基前列腺素脱氢酶氧化，这与YPG-209在体内相对持久的支气管扩张活性一致。
