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Discovery of a G Protein-Biased Radioligand for the Histamine H2 Receptor with Reversible Binding Properties

Tropmann, Katharina ; Höring, Carina ; Plank, Nicole ; Pockes, Steffen


Currently employed histamine H-2 receptor (H2R) radioligands possess several drawbacks, for example, high nonspecificity, insurmountable binding, or short half-life. We report the synthesis and the chemical and pharmacological characterization of the highly stable carbamoylguanidine-type radioligand [H-3]UR-KAT479 ([H-3]23), a subtype selective histamine H-2 receptor G protein-biased agonist. ...


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