Discovery of Potential, Dual-Active Histamine H₃ Receptor Ligands with Combined Antioxidant Properties.

ABSTRACT: In an attempt to find new dual acting histamine H₃ receptor (H₃R) ligands, we designed a series of compounds, structurally based on previously described in our group, a highly active and selective human histamine H₃ receptor (hH₃R) ligand KSK63. As a result, 15 obtained compounds show moderate hH₃R affinity, the best being the compound 17 (hH₃R K_i = 518 nM). Docking to the histamine H₃R homology model revealed two possible binding modes, with key interactions retained in both cases. In an attempt to find possible dual acting ligands, selected compounds were tested for antioxidant properties. Compound 16 (hH₃R K_i = 592 nM) showed the strongest antioxidant

SUBMITTER: Kuder KJ 

PROVIDER: S-EPMC8071534 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature