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The following message was posted to: PharmPK
I would like to know about the preferential activity of (S)(+) ibuprofen
over the racemic ibuprofen and R -isomer. I wolud appreciate if any one can
pass on the information on COX-2 IC (subscript: 50) / COX-1 IC
(subscript: 50) ratios for S(+)Ibuprofen and racemic Ibuprofen.
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The following message was posted to: PharmPK
Dear Sir
Concerning your question on IC50 values for ibuprofen on COX-1 and COX-2
activity, there are several reports for the racemate, but I just have one
for S(+) enantiomer. I have not data on R(-) enantiomers, this could be due
to the metabolic chiral inversion of R(-)IBP to S(+)IBP in human beings.
I can give you some data on racemate, however you must consider the
important differences between values depending on the technique applied and
also if the cells used are intact or broken:
IC50 COX-1 (broken cell): 3 =B5g/ml
IC50 COX-1 (intact cell): 1 =B5g/ml
IC50 COX-1 (purified enzyme): 3 =B5g/ml
IC50 COX-2 (broken cell): 160 =B5g/ml
IC50 COX-2 (intact cell): 15 =B5g/ml
IC50 COX-2 (purified enzyme): 46 =B5g/ml
This data are from Mitchell et al, Proc.Natl Acad.Sci.USA (1993) 90:
11693-11697
=46or the pure S(+)enantiomer I can give only the following data:
IC50 for COX-1: 8.9 - 14 =B5M
IC50 for COX-2: 7.2 - 8.2 =B5M
This data are from Meade et al., J.Biol.Chem. (1993) 268: 6610-6614.
Another interesting source of information is:
Vane ,J.; Botting, R. (1998) Clinical significance and potential of
selective COX-2 inhibitors. William Harvey Press, London
There much more data and in fact our group is working in the subject, if
you feel so please contact me and we can have a nice discussion.
I hope it helps.
Fabiana
Prof. Dra Maria Fabiana Landoni, PhD
Catedra de Farmacologia.
=46acultad de Ciencias Veterinarias
Universidad Nacional de La Plata
=46AX +54-221-425-7980
Calle 60 y 118 cc 296
(1900) La Plata.
ARGENTINA
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