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L-745,337:一种环氧化酶-2的选择性抑制剂可引发大鼠的抗伤害感受但不会导致胃溃疡。

L-745,337: a selective inhibitor of cyclooxygenase-2 elicits antinociception but not gastric ulceration in rats.

作者信息

Boyce S, Chan C C, Gordon R, Li C S, Rodger I W, Webb J K, Rupniak N M, Hill R G

机构信息

Merck Sharp and Dohme Research Laboratory, Neuroscience Research Centre, Terlings Park, Harlow, Essex, U.K.

出版信息

Neuropharmacology. 1994 Dec;33(12):1609-11. doi: 10.1016/0028-3908(94)90137-6.

DOI:10.1016/0028-3908(94)90137-6
PMID:7760984
Abstract

L-745,337 [5-methanesulphonamido-6-(2,4-difluorothiophenyl)-1-indan one] a selective cyclooxygenase-2 inhibitor reversed hyperalgesia induced by carrageenan in rats without causing gastric ulceration at doses 100 times those causing antinociception. In contrast, piroxicam and indomethacin produced ulcerations at antinociceptive doses. These findings demonstrate that L-745,337 possesses antinociceptive activity but has a reduced liability for gastric ulceration.

摘要

L-745,337[5-甲磺酰胺基-6-(2,4-二氟噻吩基)-1-茚酮],一种选择性环氧化酶-2抑制剂,能逆转角叉菜胶诱导的大鼠痛觉过敏,且在产生抗伤害感受剂量的100倍时不会引起胃溃疡。相比之下,吡罗昔康和吲哚美辛在产生抗伤害感受的剂量时会导致溃疡。这些发现表明,L-745,337具有抗伤害感受活性,但导致胃溃疡的可能性降低。

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1
L-745,337: a selective inhibitor of cyclooxygenase-2 elicits antinociception but not gastric ulceration in rats.L-745,337:一种环氧化酶-2的选择性抑制剂可引发大鼠的抗伤害感受但不会导致胃溃疡。
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2
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Selective cyclo-oxygenase-2 inhibition with celecoxib elevates blood pressure and promotes leukocyte adherence.塞来昔布对环氧化酶-2的选择性抑制作用会升高血压并促进白细胞黏附。
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Limited anti-inflammatory efficacy of cyclo-oxygenase-2 inhibition in carrageenan-airpouch inflammation.环氧化酶-2抑制在角叉菜胶气囊肿炎症中的抗炎效果有限。
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