Key result
S-ibuprofen inhibited PGHS-1 and PGHS-2 equally (IC50 2.1 and 1.6 microM), while R-ibuprofenoyl-CoA thioester potently inhibited PGHS-2 induction (IC50 5.6 microM).
S-ibuprofen is the active enantiomer for cyclo-oxygenase inhibition, but R-ibuprofenoyl-CoA thioester also contributes to therapeutic effects by inhibiting PGHS-2 induction.
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May add to ibuprofen's anti-inflammatory actions via R-metabolite; animal data leave open human translation.
Neupert et al. (1997) studied this question. Ibuprofen enantiomers and coenzyme A thioesters was evaluated on Inhibition of cyclo-oxygenase activity of PGHS-1 and PGHS-2. S-ibuprofen inhibited PGHS-1 and PGHS-2 equally (IC50 2.1 and 1.6 microM), while R-ibuprofenoyl-CoA thioester potently inhibited PGHS-2 induction (IC50 5.6 microM).
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