Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
Article Details
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Riendeau D, Salem M, Styhler A, Ouellet M, Mancini JA, Li CS
Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1201-3.
- PubMed ID
- 14980665 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Loxoprofen Prostaglandin G/H synthase 1 Protein Humans YesAntagonistDetails Loxoprofen Prostaglandin G/H synthase 2 Protein Humans YesAntagonistDetails - Binding Properties
Drug Target Property Measurement pH Temperature (°C) Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 440 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 730 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 530 N/A N/A Details