Boyce S, Chan C C, Gordon R, Li C S, Rodger I W, Webb J K, Rupniak N M, Hill R G
Merck Sharp and Dohme Research Laboratory, Neuroscience Research Centre, Terlings Park, Harlow, Essex, U.K.
Neuropharmacology. 1994 Dec;33(12):1609-11. doi: 10.1016/0028-3908(94)90137-6.
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.
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。