对洛索洛芬及其醇代谢物抑制环氧化酶-2的效力和选择性进行评估。
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
作者信息
Riendeau Denis, Salem Myriam, Styhler Angela, Ouellet Marc, Mancini Joseph A, Li Chun Sing
机构信息
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Quebec, Canada H9H 3L1.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3. doi: 10.1016/j.bmcl.2003.12.047.
PMID:14980665
Abstract
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.
摘要
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。
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