The partial agonist properties of levocabastine in neurotensin-induced analgesia

  • Dubuc I
  • Remande S
  • Costentin J
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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.

Author-supplied keywords

  • Analgesia
  • Hypothermia
  • Levocabastine
  • Neurotensin
  • Neurotensin low affinity receptor

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Authors

  • Isabelle Dubuc

  • Sandra Remande

  • Jean Costentin

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