Trisubstituted 1,3,5-Triazines as Histamine H₄ Receptor Antagonists with Promising Activity In Vivo.

ABSTRACT: Pain is a very unpleasant experience that makes life extremely uncomfortable. The histamine H₄ receptor (H₄R) is a promising target for the treatment of inflammatory and immune diseases, as well as pain. H₄R ligands have demonstrated analgesic effects in a variety of pain models, including inflammatory pain. Continuing the search for active H₄R ligands among the alkyl derivatives of 1,3,5-triazine, we obtained 19 new compounds in two series: acyclic (I) and aliphatic (II). In vitro pharmacological evaluation showed their variable affinity for H₄R. The majority of compounds showed a moderate affinity for this receptor (K_i > 100 nM), while all compounds tested in ß-arrestin and cAMP assays showed antagonistic activity. The mos

SUBMITTER: Olejarz-Maciej A 

PROVIDER: S-EPMC10224356 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature