前列腺素拮抗剂的研究。
Studies on prostaglandin antagonists.
作者信息
Bennett A, Posner J
出版信息
Br J Pharmacol. 1971 Aug;42(4):584-94. doi: 10.1111/j.1476-5381.1971.tb07142.x.
Abstract
- Three prostaglandin antagonists have been examined for their ability to block PGE(2) and PGF(2alpha) on human, guinea-pig and isolated rat gastrointestinal muscle.2. 7-oxa-13-Prostynoic acid was either a non-selective antagonist, or was ineffective on the tissues studied; it had marked spasmogenic activity on the rat fundus.3. 1-Acetyl-2-(8-chloro-10,11-dihydrodibenz (b,f)(1,4) oxazepine-10-carbonyl) hydrazine selectively antagonized the excitatory effects of PGE(2) and PGF(2alpha) in guinea-pig and rat tissues, but not in human muscle.4. Polyphloretin phosphate selectively antagonized the excitatory effects of prostaglandins in both human and guinea-pig muscle preparations, but it caused stimulation of the rat fundus.5. All the antagonists lowered the tone in many tissues. They also reduced contractions caused by potassium.6. None of the compounds blocked the inhibitory effect of PGE(2) on intestinal circular muscle.7. The implication of these results on the nature of prostaglandin receptors, and the value of each compound as a prostaglandin antagonist are discussed.
摘要
已对三种前列腺素拮抗剂在人、豚鼠及离体大鼠胃肠道肌肉上阻断前列腺素E2（PGE2）和前列腺素F2α（PGF2α）的能力进行了研究。
7-氧杂-13-前列腺炔酸要么是一种非选择性拮抗剂，要么对所研究的组织无效；它对大鼠胃底有明显的致痉挛活性。
1-乙酰基-2-（8-氯-10,11-二氢二苯并（b,f）（1,4）恶唑嗪-10-羰基）肼选择性地拮抗PGE2和PGF2α对豚鼠和大鼠组织的兴奋作用，但对人体肌肉无效。
聚磷酸根皮苷选择性地拮抗前列腺素对人体和豚鼠肌肉制剂的兴奋作用，但它会刺激大鼠胃底。
所有拮抗剂均降低了许多组织的张力。它们还减少了由钾引起的收缩。
这些化合物均未阻断PGE2对肠环行肌的抑制作用。
讨论了这些结果对前列腺素受体性质的意义以及每种化合物作为前列腺素拮抗剂的价值。
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