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Dimeric carbamoylguanidine-type histamine H2 receptor ligands: A new class of potent and selective agonists

Kagermeier, Nicole ; Werner, Kristin ; Keller, Max ; Baumeister, Paul ; Bernhardt, Günther ; Seifert, Roland ; Buschauer, Armin


The bioisosteric replacement of the acylguanidine moieties in dimeric histamine H2 receptor (H2R) agonists by carbamoylguanidine groups resulted in compounds with retained potencies and intrinsic activities, but considerably improved stability against hydrolytic cleavage. These compounds achieved up to 2500 times the potency of histamine when studied in [35S]GTPγS assays on recombinant human and ...


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