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与前列腺素合成抑制剂和吗啡相比,吡啶并嘧啶衍生物利马唑ium的镇痛和抗炎作用分析。

Analysis of the analgesic and anti-inflammatory effects of rimazolium, a pyrido-pyrimidine derivative, compared with that of prostaglandin synthesis inhibitors and morphine.

作者信息

Gyires K, Fürst S, Miklya I, Budavari I, Knoll J

出版信息

Drugs Exp Clin Res. 1985;11(8):493-500.

PMID:3879753
Abstract

The analgesic, anti-inflammatory and gastrointestinal effects of rimazolium, morphine and prostaglandin synthesis inhibitors were compared in a battery of tests. Rimazolium, morphine and indomethacin all inhibited carrageenin-induced inflammation; however, the onset of action was different. The first (histamine-serotonin) phase was inhibited by rimazolium, the second (kinin) phase by morphine and the third (prostaglandin) by indomethacin. The chemoluminescence of leucocytes was inhibited by morphine and indomethacin but was unaffected by rimazolium. Prostaglandin-mediated pain (ACh, ATP, acetic acid writhing) was inhibited by all three types of compound; however, pain reaction where prostaglandins (PGs) are not involved (MgSO4 writhing) was inhibited by rimazolium and morphine, but not (or only slightly) by PG synthesis inhibitors. Gastric lesions produced by indomethacin were depressed by rimazolium and aggravated by morphine. These results suggest different mechanisms of anti-inflammatory and analgesic action of rimazolium, morphine and PG synthesis inhibitors.

摘要

在一系列试验中比较了利马唑铵、吗啡和前列腺素合成抑制剂的镇痛、抗炎及胃肠道作用。利马唑铵、吗啡和吲哚美辛均能抑制角叉菜胶诱导的炎症;然而,它们的起效时间不同。第一阶段(组胺-血清素阶段)的炎症被利马唑铵抑制,第二阶段(激肽阶段)被吗啡抑制,第三阶段(前列腺素阶段)被吲哚美辛抑制。吗啡和吲哚美辛可抑制白细胞的化学发光,但利马唑铵对其无影响。三种化合物均能抑制前列腺素介导的疼痛(乙酰胆碱、三磷酸腺苷、醋酸扭体反应);然而,不涉及前列腺素(PGs)的疼痛反应(硫酸镁扭体反应)可被利马唑铵和吗啡抑制,但PG合成抑制剂对此无抑制作用(或仅有轻微抑制作用)。吲哚美辛所致的胃损伤可被利马唑铵减轻,被吗啡加重。这些结果提示利马唑铵、吗啡和PG合成抑制剂的抗炎及镇痛作用机制不同。

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