Synthesis and functional characterization of imbutamine analogs as histamine H3 and H4 receptor ligands

…, M Kaske, P Baumeister, A Buschauer

Index: Geyer, Roland; Kaske, Melanie; Baumeister, Paul; Buschauer, Armin Archiv der Pharmazie, 2014 , vol. 347, # 2 p. 77 - 88

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Citation Number: 6

Abstract

Imbutamine (4-(1H-imidazol-4-yl) butanamine) is a potent histamine H3 (H3R) and H4 receptor (H4R) agonist (EC50 values: 3 and 66nM, respectively). Aiming at improved selectivity for the H4R, the imidazole ring in imbutamine was methyl-substituted or replaced by various differently substituted heterocycles (1, 2, 3-triazoles, 1, 2, 4-triazoles, pyridines, pyrimidines) as potential bioisosteres. Investigations in [35S] GTPgS binding assays using ...