Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2.

Article Details

Citation

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
DrugTargetKindOrganismPharmacological ActionActions
LoxoprofenProstaglandin G/H synthase 1ProteinHumans
Yes
Antagonist
Details
LoxoprofenProstaglandin G/H synthase 2ProteinHumans
Yes
Antagonist
Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)440N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)730N/AN/ADetails
RofecoxibProstaglandin G/H synthase 2IC 50 (nM)530N/AN/ADetails