Abstract
The ability of histamine H 3 receptor ligands to interact with 5-HT 3 receptors in NG108-15 cells was studied using the whole cell patch clamp recording technique. Imetit, a histamine H 3 receptor agonist, generated inward currents and exhibited weak partial agonist activity at the 5-HT 3 receptor (EC 50=11.8 μM). Imetit-induced currents were slow to desensitize and at a high concentration reduced in size. The histamine H 3 receptor antagonists iodophenpropit and thioperamide did not generate inward currents but were able to inhibit 5-hydroxytryptamine (5-HT) responses with an IC 50 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.
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