The human 5-ht 5A receptor couples to G i /G o proteins and inhibits adenylate cyclase in HEK 293 cells

The human 5-ht 5A receptor couples to G i /G o proteins and inhibits adenylate cyclase in HEK 293... 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png European Journal of Pharmacology Elsevier

The human 5-ht 5A receptor couples to G i /G o proteins and inhibits adenylate cyclase in HEK 293 cells

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Publisher
Elsevier
Copyright
Copyright © 1998 Elsevier Science B.V.
ISSN
0014-2999
DOI
10.1016/S0014-2999(98)00744-4
Publisher site
See Article on Publisher Site

Abstract

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.

Journal

European Journal of PharmacologyElsevier

Published: Nov 20, 1998

References

  • The 5-HT 5A serotonin receptor is expressed predominantly by astrocytes in which it inhibits cAMP accumulation: a mechanism for neuronal suppression of reactive astrocytes
    Carson, M.J.; Thomas, E.A.; Danielson, P.E.; Sutcliffe, J.G.
  • 5-HT receptor classification and nomenclature: towards a harmonization with the human genome
    Hoyer, D.; Martin, G.
  • Functional coupling of a recombinant human 5-HT 5A receptor to G-proteins in HEK-293 cells
    Hurley, P.T.; McMahon, R.A.; Fanning, P.; O'Boyle, K.M.; Rogers, M.; Martin, F.

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