The partial agonist properties of levocabastine in neurotensin-induced analgesia

Eur J Pharmacol. 1999 Sep 17;381(1):9-12. doi: 10.1016/s0014-2999(99)00554-3.

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.

MeSH terms

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

Substances

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