Table 2

Inhibition of rat and human COX-1 and COX-2 by (R,S)-, (S)-, and (R)-ketorolac

CompoundRat COX ID502-aHuman COX ID502-a
rCOX-1rCOX-2rCOX-1/rCOX-2hCOX-1hCOX-2hCOX-1/hCOX-2
μM μM
(R,S)-ketorolac0.27  ± 0.062.06  ± 0.950.131.23  ± 0.163.50  ± 0.630.35
(S)-ketorolac0.10  ± 0.080.79  ± 0.600.130.46  ± 0.081.46  ± 0.430.32
(R)-ketorolac>1002-b >1002-b >1002-b >1002-b
DS0.20  ± 0.110.60  ± 0.180.330.90  ± 1.221.50  ± 0.800.60
INDO0.22  ± 0.146.90  ± 2.000.030.66  ± 0.5614.56  ± 9.300.04
Celecoxib57.2  ± 24.90.04  ± 0.011431
  • 2-a Values are mean ± S.E. from at least three separate determinations.

  • 2-b Due to the weakness of binding, an ID50 value could not be determined.

  • 2-c Values previously reported (Ramesha, 1996).