Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain

  title={Evidence for a displaceable non-specific [3H]neurotensin binding site in rat brain},
  author={A. Schotte and J. Leysen and P. Laduron},
  journal={Naunyn-Schmiedeberg's Archives of Pharmacology},
  • A. Schotte, J. Leysen, P. Laduron
  • Published 2004
  • Biology, Medicine
  • Naunyn-Schmiedeberg's Archives of Pharmacology
  • SummaryLevocabastine is a potent antihistamine drug, structurally unrelated to neurotensin. In rat and mouse brain but not in other animal species, it inhibited 60% of the [3H]neurotensin binding displaced by unlabelled neurotensin or neurotensin (8–13).The levocabastine-sensitive site or “site 1” displayed high affinity properties for levocabastine (IC50=25 nM) and was highly stereospecific (IC50-value higher than 10 μM for one of the isomers). Binding to the “site 1” in rat brain corresponded… CONTINUE READING
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