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Mutations of Cys-17 and Ala-271 in the Human Histamine H₂
Receptor Determine the Species Selectivity of Guanidine-Type Agonists and Increase Constitutive Activity

URN to cite this document:
urn:nbn:de:bvb:355-epub-26717
Preuss, Hendrik ; Ghorai, Prasanta ; Kraus, Anja ; Dove, Stefan ; Buschauer, Armin ; Seifert, Roland
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Date of publication of this fulltext: 05 Aug 2009 13:40


Abstract

In a steady-state GTPase activity assay, N-[3-(1H-imidazol-4-yl)propyl)]guanidines and N(G)-acylated derivatives are more potent and efficacious at fusion proteins of guinea pig (gpH₂R-GsαS) than human (hH₂R-GsαS) histamine H₂ receptor, coupled to the short splice variant of Gsα, GsαS. Whereas Ala-271 (hH₂R) and Asp-271 (gpH₂R) in transmembrane domain 7 were identified to determine the potency ...

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