Riendeau Denis, Salem Myriam, Styhler Angela, Ouellet Marc, Mancini Joseph A, Li Chun Sing
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec, Canada H9H 3L1.
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3. doi: 10.1016/j.bmcl.2003.12.047.
Loxoprofen, its trans-alcohol and cis-alcohol metabolites were evaluated for selectivity of inhibition of COX-2 over COX-1. The (2S,1'R,2'S)-trans-alcohol derivative was found to be the most active metabolite and to be a potent and nonselective inhibitor of COX-2 and COX-1 in both enzyme and human whole blood assays.
对洛索洛芬及其反式醇和顺式醇代谢物进行了COX - 2相对于COX - 1抑制选择性的评估。发现(2S,1'R,2'S)-反式醇衍生物是最具活性的代谢物，并且在酶和人全血测定中都是COX - 2和COX - 1的强效非选择性抑制剂。
