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XB-ART-35950
Eur J Pharmacol 2007 Jul 19;5673:206-10. doi: 10.1016/j.ejphar.2007.04.032.
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The human histamine H3 receptor couples to GIRK channels in Xenopus oocytes.

Sahlholm K, Nilsson J, Marcellino D, Fuxe K, Arhem P.


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The histamine H(3) receptor mediates inhibitory responses in the nervous system. Here, we demonstrate the coupling of the human histamine H(3) receptor to G protein-coupled inward rectifier potassium (GIRK) channels in Xenopus oocytes, using voltage-clamp. The histamine H(3) receptor agonist (R)-alpha-methylhistamine increased GIRK currents with an EC(50) of 2.5 nM. The response to (R)-alpha-methylhistamine was inhibited by the specific antagonist/inverse agonist clobenpropit. GIRK channels represent a novel effector pathway for the histamine H(3) receptor, also suggesting the use of electrophysiology assays in histamine H(3) receptor drug screening, allowing for the resolution of G protein activation kinetics.

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Species referenced: Xenopus
Genes referenced: kcnj3