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Evaluation of 2 celecoxib derivatives:analgesic effect and selectivity to cyclooxygenase-2/1

Acta Pharmacologica Sinica 2005年第12期26卷 1505-1511页

作者： Zhi-hong LU~(2,4) Xiao-yun XIONG~2 Bang-le ZHANG~2 Guo-cheng LIN~3 Yu-xiang SHI~4 Zhen-guo LIU~2 Jing-ru MENG~2 Yu-mei ZHOU~3 Qi-bing MEI~(3,6) 2 Department of Pharmacology,3 Department of Radioactive Isotopes,and 4 Department of Anesthesiology,Xijing Hospital,Fourth Military Medical University,Xi'an 710032,China 5 Department of Foreign Languages,Fourth Military Medical University,Xi'an 710032,China Department of Pharmacology Xijing Hospital Fourth Military Medical University Xi'an China Department of Foreign Languages Fourth Military Medical University Xi'an China Department of Anesthesiology Xijing Hospital Fourth Military Medical University Xi'an China Department of Radioactive Isotopes Xijing Hospital Fourth Military Medical University Xi'an China

Aim:To evaluate the analgesic effects of 2 celecoxib derivatives and their inhibi-tory effects on cyclooxygenase（COX）.Methods:Four antinociceptive assayswere used:the acetic acid-induced writhing test,hot plate test,hot tail-flick testand formalin *** doses were used in the analgesic assays and ED50valueswere *** the selectivity assay,macrophages were incubated with testcompounds at various concentrations and then stimulated with calcimycin orlipopolysaccharide（LPS）.The amounts of 6-keto-prostaglandin F1α(6-keto-PGF1α)and prostaglandin E2（PGE2）in the supernatant were examined by radioimmunoas-say（RIA）.The selectivity of the test compounds was expressed as the ***-1/***:Celecoxib and its 2 derivatives had a significant analge-sic *** ED50values of celecoxib,PC-406 and PC-407 were 94.2,67.9,and 63.3mg/kg,respectively,for the acetic acid-induced writhing test;104.7,89.1,and 30.0mg/kg,respectively,for the hot tail-flick response test;60.7,56.7,and 86.2 mg/kg,respectively,for the hot plate response test;67.1,55.8,and 68.8 mg/kg,respectively,for the formalin-induced *** is,the EDs0 of PC-406 was the lowest forthe formalin and hot plate tests,which focus on changes above the spinal cordlevel;however,the EDs0 of PC-407 was lowest for the tail-flick and writhing tests,which focus on changes at the spinal cord *** and PC-407 inhibitedCOX-1 with IC50values of 39.8 and 27.5 nmol/L,***-406 inhibitedCOX-1 with an IC50value of more than 1000 nmol/*** IC50values for the effectof celecoxib,PC-406 and PC-407 on COX-2 were 4.8,8.9,and 1.9 nmol/L *** ***-1]***-2ratios for celecoxib and PC-407 were 8.3 and 14.4,*** PC-406,the ratio was greater than ***:Derivatives ofcelecoxib via substitution with an isopropyl or naphthyl group at the 5 position inthe pyrazole ring still have analgesic effects and the ability to selectively *** wit

关键词： cyclooxygenase inhibitors celecoxib pain selectivity mice

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