Agonist and antagonist effects of histamine H3 receptor ligands on 5-HT3 receptor-mediated ion currents in NG108-15 cells

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Abstract

The ability of histamine H3 receptor ligands to interact with 5-HT3 receptors in NG108-15 cells was studied using the whole cell patch clamp recording technique. Imetit, a histamine H3 receptor agonist, generated inward currents and exhibited weak partial agonist activity at the 5-HT3 receptor (EC50=11.8 μM). Imetit-induced currents were slow to desensitize and at a high concentration reduced in size. The histamine H3 receptor antagonists iodophenpropit and thioperamide did not generate inward currents but were able to inhibit 5-hydroxytryptamine (5-HT) responses with an IC50 of 1.57±0.3 μM and 13.7±3.5 μM, respectively. Thioperamide is probably a non-competitive antagonist which may have more than one binding site on the receptor. Copyright (C) 1998 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)261-268
Number of pages8
JournalEuropean Journal of Pharmacology
Volume361
Issue number2-3
DOIs
Publication statusPublished - 20 Nov 1998

Keywords

  • 5-HT receptor
  • Histamine H receptor ligand
  • Imetit
  • Iodophenpropit
  • NG108-15 cell
  • Thioperamide

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