The partial agonist properties of levocabastine in neurotensin-induced analgesia.

Abstract

The antihistaminic drug levocabastine is a ligand for the low affinity neurotensin receptor (NTS2). Its intracerebroventricular administration to mice induced a significant analgesia in the writhing test but not in the hot plate test. In the writhing test, levocabastine decreased neurotensin-induced analgesia to a level not significantly different from the effects of levocabastine alone. In the hot plate test, levocabastine had no analgesic effect but completely reversed the neurotensin-induced analgesia. Mepyramine, another antihistaminic drug, did not share these levocabastine effects. Neither levocabastine nor mepyramine modified the colonic temperature or reversed the neurotensin-induced hypothermia. Thus, levocabastine behaves as a partial agonist at neurotensin NTS2 receptors, which are involved in visceral nociception, but not at yet unidentified neurotensin receptors involved in hypothermia.

• Authors: I Dubuc, S Remande, J Costentin
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 381 Issue 1 Pg. 9-12 (Sep 17 1999) ISSN: 0014-2999 [Print] Netherlands
• PMID: 10528128 (Publication Type: Journal Article)

Chemical References

• Analgesics
• Histamine H1 Antagonists
• Piperidines
• Receptors, Neurotensin
• Neurotensin
• levocabastine
• Pyrilamine

Topics

• Analgesia
• Analgesics (pharmacology)
• Animals
• Dose-Response Relationship, Drug
• Histamine H1 Antagonists (pharmacology)
• Male
• Mice
• Neurotensin (pharmacology)
• Pain (chemically induced, prevention & control)
• Pain Threshold (drug effects)
• Piperidines (pharmacology)
• Pyrilamine (pharmacology)
• Receptors, Neurotensin (agonists)