Antinociception by fluoro-loxoprofen, a novel non-steroidal anti-inflammatory drug with less ulcerogenic effects, in rat models of inflammatory pain
Antinociception by fluoro-loxoprofen, a novel non-steroidal anti-inflammatory drug with less ulcerogenic effects, in rat models of inflammatory pain
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氟洛索洛芬（一种新型非甾体抗炎药，具有较少的溃疡形成作用）在大鼠炎性疼痛模型中的镇痛作用
DOI：
10.1016/j.ejphar.2018.12.008
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发表时间：
2019
影响因子：
5
通讯作者：
Takenaga Mitsuko
中科院分区：
文献类型：
--
作者：
Asano Teita;Hattori Tomoki;Tanaka Ken-ichiro;Yamakawa Naoki;Suemasu Shintaro;Aida Shuji;Kataoka Marika;Mizushima Tohru;Takenaga Mitsuko
使用非甾体抗炎药（NSAID）治疗炎性疼痛受到胃肠道并发症的限制。NSAID的快速作用与更好的疼痛缓解相关。以前，我们证明了氟洛索洛芬，一种新的NSAID，具有较低的溃疡潜力比其他NSAID，归因于其胃保护性能。本研究的目的是调查和比较氟洛索洛芬对大鼠炎性疼痛的影响与其他非甾体抗炎药。氟洛索洛芬、洛索洛芬和塞来昔布的口服给药对酵母诱导的炎性疼痛具有等效的镇痛作用。氟洛索洛芬的抗伤害作用在给药后1 h内达到最大，这比洛索洛芬（2 h）和塞来昔布（3 h）观察到的时间短。我们证实氟洛索洛芬和洛索洛芬都能抑制发炎爪子中前列腺素E2的增加。除了酵母诱导的疼痛外，氟洛索洛芬对促炎剂诱导的炎性疼痛也产生了类似的作用，其镇痛作用峰值比洛索洛芬和塞来昔布更快。综上所述，这些结果表明氟洛索洛芬的镇痛作用与洛索洛芬和塞来昔布相当。此外，氟洛索洛芬对炎性疼痛的镇痛作用比其他NSAID更迅速，这可能与其快速吸收特性有关。
The use of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammatory pain is limited by gastrointestinal complications. The rapid action of NSAIDs is associated with better pain relief. Previously, we demonstrated that fluoro-loxoprofen, a novel NSAID, has less ulcerogenic potential than other NSAIDs, attributable to its gastroprotective properties. The aim of this study was to investigate and compare the effects of fluoro-loxoprofen on inflammatory pain in rats with those of other NSAIDs. Oral administration of fluoro-loxoprofen, loxoprofen, and celecoxib resulted in equivalent analgesic action against yeast-induced inflammatory pain. The antinociceptive effect of fluoro-loxoprofen was maximized within 1 h after administration, which is less time than that observed for loxoprofen (2 h) and celecoxib (3 h). We confirmed that both fluoro-loxoprofen and loxoprofen suppressed the increases in prostaglandin E2in inflamed paws. In addition to yeast-induced pain, fluoro-loxoprofen produced a similar effect against adjuvant-induced inflammatory pain, with faster peak analgesic effects than those observed for loxoprofen and celecoxib. Taken together, these results suggest that the analgesic effect of fluoro-loxoprofen is equivalent to that of loxoprofen and celecoxib. Moreover, the analgesic effect of fluoro-loxoprofen against inflammatory pain was more rapid than that of other NSAIDs, and this may be associated with its rapid absorption property.