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Point Mutations in the Second Extracellular Loop of the Histamine H2 Receptor do not affect the Species-Selective Activity of Guanidine-Type Agonists.

Preuss, Hendrik ; Ghorai, Prasanta ; Kraus, Anja ; Dove, Stefan ; Buschauer, Armin ; Seifert, Roland
Date of publication of this fulltext: 05 Aug 2009 13:42


Abstract

Residues in the second extracellular loop (e2) play a role in ligand binding in certain aminergic G protein coupled receptors (GPCRs). N-[3-(1H-Imidazol-4-yl)propyl)]guanidines and N G-acylated derivatives are more efficacious and potent agonists at fusion proteins of the guinea pig histamine H2 receptor and the short splice variant of Gsα, GsαS (gpH2R-GsαS) than at the human isoform ...

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