The G protein coupling of human 5-hydroxytryptamine 5A (h5-ht 5A ) receptors was investigated in stably transfected human embryonic kidney (HEK) 293 cells, using radioligand and guanosine-5′(γ- 35 S )thiotriphosphate binding to membranes and cyclic adenosine monophosphate measurements in cells. 5-Carboxamido( 3 H )tryptamine bound to high- and low-affinity sites on h5-ht 5A -HEK 293 cell membranes. Guanylyl-imidodiphosphate addition and pertussis toxin pre-treatment abolished high-affinity binding, indicating coupling to G proteins of the G i /G o family. ( N -methyl- 3 H )Lysergic acid diethylamide bound to a single site; guanylyl-imidodiphosphate and pertussis toxin did not alter lysergic acid diethylamide affinity. 5-Hydroxytryptamine stimulated guanosine-5′(γ- 35 S )thiotriphosphate binding to 130% over basal and this effect was completely abolished by pertussis toxin. Various 5-hydroxytryptamine receptor ligands were tested for inhibition of 5-carboxamido( 3 H )tryptamine binding and in guanosine-5′(γ- 35 S )thiotriphosphate binding assays. 5-Hydroxytryptamine consistently inhibited forskolin-induced cyclic adenosine monophosphate formation by 25% in h5-ht 5A -HEK 293 cells; no effect was detected on basal cyclic adenosine monophosphate levels, on intracellular Ca 2+ concentration or arachidonic acid release. Our studies demonstrate functional coupling of the h5-ht 5A receptor to pertussis toxin-sensitive G proteins and to inhibition of adenylate cyclase activity.
European Journal of Pharmacology – Elsevier
Published: Nov 20, 1998
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