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Multiple differences in agonist and antagonist pharmacology between human and guinea pig histamine H1-receptor,

Seifert, Roland ; Wenzel-Seifert, Katharina ; Bürckstümmer, Tilmann ; Pertz, Heinz H. ; Schunack, Walter ; Dove, Stefan ; Buschauer, Armin ; Elz, Sigurd



Abstract

Species isoforms of histamine H2-, H3-, and H4-receptors differ in their pharmacological properties. The study aim was to dissect differences between the human H1R (hH1R) and guinea pig H1R (ghH1R). We coexpressed hH1R and gpH1R with regulators of G-protein signaling in Sf9 insect cells and analyzed the GTPase activity of Gq-proteins. Small H1R agonists showed similar effects at hH1R and gpH1R, ...

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