Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates

A series of imidazole-containing (non-)chiral carbamates were tested at human histamine H3 receptor (H3R). All compounds displayed Ki values below 100 nM. A trend for a stereoselectivity at human H3R was observed for the chiral α-branched ligands. Selected compounds were also tested at human histamine H4 receptor and showed moderate to weak affinities (118–1460 nM).

Branched 3-(1H-imidazol-4-yl)propyl alkylcarbamates were investigated at the human histamine H3 receptor (CHO-K1 or HEK-293 cells). A trend for a stereoselectivity at human H3R was observed for the chiral α-branched ligands. Selected compounds were also tested at the human histamine H4 receptor (Sf9 cells).Figure optionsDownload as PowerPoint slide