Zaltoprofen, a non-steroidal anti-inflammatory drug, inhibits bradykinin-induced pain responses without blocking bradykinin receptors
| Autor: | Yuki Ogawa, Kentaro Yoda, Aoi Uchida, Kenji Hirate, Tomoko Arai |
|---|---|
| Rok vydání: | 2006 |
| Předmět: |
Male
Receptor Bradykinin B2 Guinea Pigs Pain Bradykinin In Vitro Techniques Pharmacology Receptor Bradykinin B1 Mice Radioligand Assay chemistry.chemical_compound Mofezolac Ganglia Spinal medicine Animals Benzopyrans Cyclooxygenase Inhibitors Rats Wistar Etodolac Receptor Bradykinin Receptor Antagonists Cells Cultured Acetic Acid Mice Inbred ICR biology Receptors Bradykinin General Neuroscience Anti-Inflammatory Agents Non-Steroidal Antagonist General Medicine Loxoprofen Rats Meloxicam chemistry biology.protein Calcium Cyclooxygenase Propionates medicine.drug |
| Zdroj: | Neuroscience Research. 54:288-294 |
| ISSN: | 0168-0102 |
| Popis: | Zaltoprofen, a preferential COX-2 inhibitor, exhibited a potent inhibitory action on the nociceptive responses induced by a retrograde infusion of bradykinin into the right common carotid artery in rats. However, other COX-2 preferential inhibitors such as meloxicam and etodolac did not exhibit any apparent action, and also, preferential COX-1 inhibitors mofezolac and indomethacin, COX-1 and COX-2 inhibitor loxoprofen sodium showed a weak effect. These non-steroidal anti-inflammatory drugs (NSAIDs) except for zaltoprofen, strongly inhibited an acetic acid-induced writhing response related to PGs based on COX-1, at lower doses. Zaltoprofen had a moderate inhibitory effect compared with those of the above-mentioned NSAIDs. These results suggest that the inhibitory effect of zaltoprofen on bradykinin-induced nociceptive responses is not explainable by the inhibition of cyclooxygenase (COX). So, we examined the inhibitory effect of zaltoprofen on bradykinin-induced nociceptive responses by performing several in vitro experiments. Zaltoprofen did not bind to B 1 and B 2 receptors in a radio-ligand binding assay. In the cultured dorsal root ganglion cells of mature mice, zaltoprofen completely inhibited the bradykinin-induced increase of [Ca 2+ ] i , which was inhibited by B 2 antagonist D-Arg-[Hyp 3 , Thi 5,8 , D-Phe 7 ]-bradykinin, but not by B 1 antagonist. In addition, the inhibition of zaltoprofen on the increase of [Ca 2+ ] i was observed even under extracellular Ca 2+ -free conditions. The above results suggest that zaltoprofen produces an analgesic action on bradykinin-induced nociceptive responses by blocking the B 2 receptor-mediated pathway in the primary sensory neurons. Taken together, these results suggest that zaltoprofen may serve as a potent and superior analgesic for the treatment of pain. |
| Databáze: | OpenAIRE |
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