ASPIRIN-LIKE DRUGS MAY BLOCK PAIN INDEPENDENTLY OF PROSTAGLANDIN SYNTHESIS INHIBITION

被引:145
作者
BRUNE, K [1 ]
BECK, WS [1 ]
GEISSLINGER, G [1 ]
MENZELSOGLOWEK, S [1 ]
PESKAR, BM [1 ]
PESKAR, BA [1 ]
机构
[1] RUHR UNIV BOCHUM,DEPT PHARMACOL & TOXICOL,W-4630 BOCHUM 1,GERMANY
来源
EXPERIENTIA | 1991年 / 47卷 / 03期
关键词
ASPIRIN-LIKE DRUGS; FLURBIPROFEN ENANTIOMERS; ANTIINFLAMMATORY; ANALGESIC; GASTROINTESTINAL TOXICITY; PROSTAGLANDIN SYNTHESIS; RAT;
D O I
10.1007/BF01958153
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Using flurbiprofen, a chiral anti-inflammatory and analgesic 2-arylpropionic acid derivative, the enantiomers of which are not converted to each other (less than 5%) in rats or man, we obtained evidence that prostaglandin synthesis inhibition is primarily mediating the anti-inflammatory activity but prostaglandin synthesis independent mechanisms contribute to the analgesic effects. Thus, the S-form inhibited prostaglandin synthesis, inflammation and nociception in rats. The R-form had much less effect on prostaglandin synthesis and did not affect inflammation. It did, however, block nociception in rats almost as potently as the S-form. S-flurbiprofen, in contrast to the R-form, was clearly ulcerogenic in the gastrointestinal mucosa. These results indicate additional molecular mechanisms of analgesia and suggest the use of R-arylpropionic acids as analgesics.
引用
收藏
页码:257 / 261
页数:5
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