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前列腺素E1衍生物ONO-802对平滑肌的生物学活性(作者译)

[Biological activity of prostaglandin E1 derivative, ONO-802 on smooth muscle (author's transl)].

作者信息

Mori N, Iwasa T, Kawano M

出版信息

Acta Obstet Gynaecol Jpn. 1981 Feb;33(2):187-92.

PMID:7234331
Abstract

The effects of prostaglandin (PG) E1 derivative, 16,16-dimethyl-trans-delta-2PGE1 methyl ester (ONO-802) on the rat stomach fundal strip, uterus and ileum were studied. Its substrate specificity for 15-hydroxy prostaglandin dehydrogenase (PGDH) was also examined. Contractions were recorded isometrically by superfusion method. PGE1, E2, and F2 alpha caused maximal contraction of the fundal strip immediately after application and relaxation to the original state within 10 min. Contractile pattern of the fundal strip produced by ONO-802 was quite specific and different from those by classic PGs. Contraction was increased slowly to its maximum in 10 to 20 min after application of ONO-802 and thereafter returned to the original state in 20 to 40 min. Contractive response of the rat ileum to ONO-802 was a gradual increase of the tonus and restoration in more than 120 min after reaching its maximal tonus. The rat uterus responded to 1 microgram of ONO-802 with double maximal contraction amplitude of spontaneous activity, with increased contraction amplitude restored in 90 min. In a combination of ONO-802 with PGE1, E2 and F2 alpha, the contractile response of the fundal strip to ONO-802 was masked by the actions of classic PGs and additional potentiation was not observed. Contractive activity of ONO-802 was not reduced by placental PGDH.

摘要

研究了前列腺素(PG)E1衍生物16,16 - 二甲基 - 反式 - δ2 - PGE1甲酯(ONO - 802)对大鼠胃底条、子宫和回肠的作用。还检测了其对15 - 羟基前列腺素脱氢酶(PGDH)的底物特异性。通过灌流法等长记录收缩情况。PGE1、E2和F2α在应用后立即引起胃底条最大收缩,并在10分钟内松弛至原始状态。ONO - 802产生的胃底条收缩模式非常特殊,与经典前列腺素不同。应用ONO - 802后10至20分钟,收缩缓慢增加至最大值,此后在20至40分钟内恢复到原始状态。大鼠回肠对ONO - 802的收缩反应是张力逐渐增加,并在达到最大张力后120多分钟恢复。大鼠子宫对1微克ONO - 802的反应是自发活动的最大收缩幅度加倍,收缩幅度增加后在90分钟内恢复。在ONO - 802与PGE1、E2和F2α的组合中,胃底条对ONO - 802的收缩反应被经典前列腺素的作用掩盖,未观察到额外的增强作用。胎盘PGDH未降低ONO - 802的收缩活性。

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