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Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H2R and D3R

Biselli, Sabrina ; Bresinsky, Merlin ; Tropmann, Katharina ; Forster, Lisa ; Honisch, Claudia ; Buschauer, Armin ; Bernhardt, Günther ; Pockes, Steffen



Abstract

Even today, the role of the histamine H-2 receptor (H2R) in the central nervous system (CNS) is widely unknown. In previous research, many dimeric, high-affinity and subtype-selective carbamoylguanidine-type ligands such as UR-NK22 (5, pK(i) = 8.07) were reported as H2R agonists. However, their applicability to the study of the H2R in the CNS is compromised by their molecular and pharmacokinetic ...

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