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Abolishing Dopamine D2long/D3 Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H2 Receptor Agonists

Tropmann, Katharina ; Bresinsky, Merlin ; Forster, Lisa ; Mönnich, Denise ; Buschauer, Armin ; Wittmann, Hans-Joachim ; Hübner, Harald ; Gmeiner, Peter ; Pockes, Steffen ; Strasser, Andrea


3-(2-Amino-4-methylthiazol-5-yl)propyl-substituted carbamoylguanidines are potent, subtype-selective histamine H-2 receptor (H2R) agonists, but their applicability as pharmacological tools to elucidate the largely unknown H2R functions in the central nervous system (CNS) is compromised by their concomitant high affinity toward dopamine D-2-like receptors (especially to the D3R). To improve the ...


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