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Dibenzo[ b , f ][1,4]oxazepines and dibenzo[ b , e ]oxepines: Influence of the chlorine substitution pattern on the pharmacology at the H 1 R, H 4 R, 5-HT 2A R and other selected GPCRs

Naporra, Franziska ; Gobleder, Susanne ; Wittmann, Hans-Joachim ; Spindler, Julia ; Bodensteiner, Michael ; Bernhardt, Günther ; Hübner, Harald ; Gmeiner, Peter ; Elz, Sigurd ; Strasser, Andrea



Abstract

Inspired by VUF6884 (7-Chloro-11-(4-methylpiperazin-1-yl)dibenzo[bf][1,4]oxazepine), reported as a dual H-1/H-4 receptor ligand (pK(i): 8.11 (human H1R (hH(1)R)), 7.55 (human H4R (hH(4)R))), four known and 28 new oxazepine and related oxepine derivatives were synthesised and pharmacologically characterized at histamine receptors and selected aminergic GPCRs. In contrast to the oxazepine series, ...

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