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Synthesis and histamine H3 and H4 receptor activity of conformationally restricted cyanoguanidines related to UR-PI376

Geyer, Roland ; Buschauer, Armin



Abstract

Recently, we identified highly potent agonists of the human histamine H4 receptor (hH4R) among a series of imidazolylbutylcyanoguanidines. Aiming at improved selectivity for the hH4R relative to the H3 receptor (hH3R), the flexible tetramethylene linker connecting imidazole ring and cyanoguanidine group was replaced by conformationally restricted carbocycles. Introduction of a para- or a ...

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