Abstract | BACKGROUND AND PURPOSE: EXPERIMENTAL APPROACH: KEY RESULTS: CONCLUSIONS AND IMPLICATIONS: The similar effects of acemetacin and indomethacin on leukocyte infiltration and PG synthesis are consistent with rapid biotransformation of acemetacin to indomethacin. Some of this biotransformation may occur extra-hepatically, for instance in inflammatory exudates. Acemetacin probably exerts actions independent of conversion to indomethacin, given the different effects of these two drugs on LTB(4) production. Such differences may contribute to the relative gastric safety of acemetacin compared to indomethacin.
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Authors | A E Chávez-Piña, W McKnight, M Dicay, G Castañeda-Hernández, J L Wallace |
Journal | British journal of pharmacology
(Br J Pharmacol)
Vol. 152
Issue 6
Pg. 930-8
(Nov 2007)
ISSN: 0007-1188 [Print] England |
PMID | 17876306
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Inflammatory Agents, Non-Steroidal
- Prostaglandins
- Thromboxanes
- Leukotriene B4
- acemetacin
- Zymosan
- Cyclooxygenase 1
- Cyclooxygenase 2
- Dinoprostone
- Indomethacin
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Topics |
- Administration, Oral
- Animals
- Anti-Inflammatory Agents, Non-Steroidal
(adverse effects, pharmacokinetics, pharmacology)
- Area Under Curve
- Biotransformation
- Chromatography, High Pressure Liquid
- Cyclooxygenase 1
(metabolism)
- Cyclooxygenase 2
(metabolism)
- Dinoprostone
(biosynthesis, genetics)
- Exudates and Transudates
(metabolism)
- Indomethacin
(adverse effects, analogs & derivatives, metabolism, pharmacokinetics, pharmacology)
- Inflammation
(chemically induced, prevention & control)
- Injections, Subcutaneous
- Leukotriene B4
(metabolism)
- Male
- Prostaglandins
(biosynthesis)
- Rats
- Rats, Wistar
- Stomach Ulcer
(chemically induced)
- Thromboxanes
(biosynthesis, blood)
- Zymosan
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