Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
Pallapies, D; Salinger, A; Meyer zum Gottesberge, A; Atkins, DJ; Rohleder, G; Nagyiványi, P; Peskar, BA.
Effects of lysine clonixinate and ketorolac tromethamine on prostanoid release from various rat organs incubated ex vivo.
Life Sci. 1995; 57(2):83-89
Doi: 10.1016%2F0024-3205%2895%2900249-6
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- Führende Autor*innen der Med Uni Graz
- Peskar Bernhard
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- Abstract:
- The release of prostanoids from rat brain, gastric mucosa, lungs and kidneys incubated ex vivo has been investigated for up to 5 h after oral administration of 10 mg/kg lysine clonixinate or 1 mg/kg ketorolac tromethamine. Additionally, 60 min after drug administration, a time point of near-maximal inhibition of prostanoid release, the effects of 2.5, 10 and 30 mg/kg lysine clonixinate and of 0.0225, 0.15 and 1 mg/kg ketorolac tromethamine were compared. In all organs investigated both drugs inhibited fatty acid cyclooxygenase (COX) in a dose-dependent manner, but ketorolac tromethamine was more potent and had a longer-lasting effect than lysine clonixinate. While the ID50 values for lysine clonixinate were in the same order of magnitude for all 4 organs investigated, ketorolac tromethamine exhibited some organ selectivity with a particularly high activity in the kidneys. This effect might be related to the renal toxicity of ketorolac tromethamine. On the other hand, the difference in potency was smallest in brain suggesting that inhibition of central prostanoid biosynthesis could contribute to the rapid and effective inhibition of pain by both drugs. IC50 values for inhibition of purified COX-1 and COX-2 in vitro were slightly lower for lysine clonixinate (2.4 and 24.6 micrograms/ml, respectively) than for ketorolac tromethamine (3.7 and 25.6 micrograms/ml, respectively).
- Find related publications in this database (using NLM MeSH Indexing)
- 6-Ketoprostaglandin F1 alpha - biosynthesis
- Administration, Oral - biosynthesis
- Analgesics - pharmacology
- Animals - pharmacology
- Anti-Inflammatory Agents, Non-Steroidal - pharmacology
- Brain - drug effects
- Clonixin - analogs and derivatives
- Cyclooxygenase Inhibitors - pharmacology
- Dinoprost - biosynthesis
- Dose-Response Relationship, Drug - biosynthesis
- Drug Combinations - biosynthesis
- Gastric Mucosa - drug effects
- Indomethacin - pharmacology
- Isoenzymes - antagonists and inhibitors
- Ketorolac Tromethamine - antagonists and inhibitors
- Kidney - drug effects
- Lung - drug effects
- Lysine - analogs and derivatives
- Male - analogs and derivatives
- Prostaglandin-Endoperoxide Synthases - metabolism
- Prostaglandins - biosynthesis
- Rats - biosynthesis
- Rats, Wistar - biosynthesis
- Thromboxane B2 - biosynthesis
- Tolmetin - analogs and derivatives
- Tromethamine - pharmacology
- Find related publications in this database (Keywords)
- Lysine Clonixinate
- Ketorolac Tromethamine
- Prostaglandin
- Thromboxane
- Cyclooxygenase