Stereoselective inhibition of rat brain cyclooxygenase by dexketoprofen

Chirality
A CarabazaD Mauleón

Abstract

Although it has been assumed that the effects of nonsteroidal antiinflammatory drugs (NSAIDs) are mainly the result of their action on local synthesis of prostaglandins, there is growing evidence to suggest that they may also exert a central analgesic action. Some authors have suggested that inhibition of prostaglandin synthesis in the brain could contribute to the analgesic action. The effect of dexketoprofen trometamol (tromethamine salt of the enantiomer (+)-S-ketoprofen) on prostaglandin synthesis was investigated in rat brain fragments and in cyclooxygenase preparations from rat brain microsomes. Effects of the (-)-R-enantiomer and the racemic mixture were also evaluated. Significant levels of prostaglandin F2 alpha (PGF2 alpha) were synthesized in rat brain fragments after 10 min of incubation at 37 degrees C. Dexketoprofen was found to be a potent inhibitor of this PGF2 alpha production in rat brain (IC50 = 6.2 nM), and it completely suppressed PGF2 alpha production at 1 microM concentration. In addition, inhibition of PGF2 alpha synthesis by dexketoprofen was highly stereoselective since the enantiomer (-)-R-ketoprofen was significantly less potent (IC50 = 294 nM); with this enantiomer, even at high concentrations such ...Continue Reading

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Citations

Apr 5, 2002·Inflammation Research : Official Journal of the European Histamine Research Society ... [et Al.]·C Alarcón de la LastraV Motilva
Mar 25, 2005·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·K H LiuJ G Shin
Dec 13, 2006·European Journal of Pharmacology·Hai-Xia QiuXing-Guo Mei
Jul 23, 2014·Knee Surgery, Sports Traumatology, Arthroscopy : Official Journal of the ESSKA·Sevtap Hekimoglu SahinNecdet Sut
Jun 14, 2005·Journal of Pharmaceutical and Biomedical Analysis·Marinko PetrovićNikola Blazević
May 28, 2014·Neurological Research·Oytun ErbaşDürdane Aksoy
Nov 6, 2020·Fundamental & Clinical Pharmacology·Lorenzo Franco de la-TorreMario Alberto Isiordia-Espinoza

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