Modulation of histamine H(3) receptor function by monovalent ions

Neuroscience Letters
David Schnell, Roland Seifert

Abstract

Monovalent ions differently affect ligand binding to G protein-coupled receptors (GPCRs) by as yet poorly defined mechanisms. In particular, NaCl often decreases the affinity of agonists but increases it for antagonists. We examined the effect of various monovalent ions on human histamine H(3) receptor (hH(3)R), co-expressed with mammalian G proteins (Galpha(i1), Galpha(i2), Galpha(i3) or Galpha(o1), and beta(1)gamma(2) dimers, respectively) in Sf9 insect cell membranes, with respect to agonist binding and G protein activation. NaCl (100mM) had no effect on affinity of the agonist [(3)H]N(alpha)-methylhistamine ([(3)H]NAMH). In steady-state GTPase assays, the endogenous agonist histamine had a lower potency and the inverse agonist thioperamide had a higher potency, when NaCl (100mM) was present. Monovalent ions reduced H(3)R-regulated signalling in the order of efficacy Li(+) approximately Na(+) approximately K(+)<Cl(-)<Br(-)<I(-). NaCl had a stronger effect on basal hH3R-signalling when Galpha(i3) was co-expressed. Asp80(2.50), a putative interaction site for Na(+), was mutated to Asn80(2.50) (D2.50N-hH(3)R). Strikingly, the mutation was unable to activate Galpha(i3) at all. The effects can be explained by a model, where (i) m...Continue Reading

References

Oct 17, 2002·Naunyn-Schmiedeberg's Archives of Pharmacology·Roland Seifert, Katharina Wenzel-Seifert
Aug 28, 2003·Life Sciences·Roland Seifert, Katharina Wenzel-Seifert
Jan 25, 2005·Nature Reviews. Drug Discovery·Rob LeursIwan J P de Esch
Jun 19, 2007·Trends in Pharmacological Sciences·Jean-Michel ArrangFlorence Gbahou
Jun 5, 2008·Naunyn-Schmiedeberg's Archives of Pharmacology·Patrick KleemannRoland Seifert
Jul 16, 2008·Physiological Reviews·Helmut L HaasOliver Selbach
Dec 5, 2009·The Journal of Pharmacology and Experimental Therapeutics·David SchnellRoland Seifert

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Citations

Mar 2, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·David SchnellRoland Seifert
Oct 29, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·Heidrun ApplRoland Seifert
Aug 8, 2014·Journal of Molecular Modeling·Hans-Joachim WittmannAndrea Strasser
Aug 8, 2014·Neuroscience and Biobehavioral Reviews·Erich H SchneiderRoland Seifert
Dec 21, 2012·Trends in Pharmacological Sciences·Roland SeifertArmin Buschauer
Nov 30, 2014·Naunyn-Schmiedeberg's Archives of Pharmacology·Andrea StrasserRoland Seifert
May 4, 2016·Scientific Reports·Taka-Aki KoshimizuJunichi Taniguchi
Jul 13, 2011·Journal of Receptor and Signal Transduction Research·Nathalie PopArmin Buschauer
Dec 1, 2014·In Silico Pharmacology·Hans-Joachim WittmannAndrea Strasser

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