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3HUR-DE257: Development of a tritium-labeled squaramide-type selective histamine H2 receptor antagonist

Baumeister, Paul ; Erdmann, Daniela ; Biselli, Sabrina ; Kagermeier, Nicole ; Elz, Sigurd ; Bernhardt, Günther ; Buschauer, Armin



Abstract

A series of new piperidinomethylphenoxypropylamine-type histamine H2 receptor (H2R) antagonists with different substituted “urea equivalents” was synthesized and characterized in functional in vitro assays. N-6-(3,4-Dioxo-2-{3-3-(piperidin-1-ylmethyl)phenoxy]-propylamino}cyclobut-1-enylamino)hexyl]-(2,3-3H2)propionic amide (3HUR-DE257, 24b) was selected for radiosynthesis. The radioligand ...

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