Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H₃ and Sigma-1 Receptor Antagonists with Promising Antinociceptive Properties.

ABSTRACT: In an attempt to extend recent studies showing that some clinically evaluated histamine H₃ receptor (H₃R) antagonists possess nanomolar affinity at sigma-1 receptors (σ₁R), we selected 20 representative structures among our previously reported H₃R ligands to investigate their affinity at σRs. Most of the tested compounds interact with both sigma receptors to different degrees. However, only six of them showed higher affinity toward σ₁R than σ₂R with the highest binding preference to σ₁R for compounds 5, 11, and 12. Moreover, all these ligands share a common structural feature: the piperidine moiety as the fundamental part of the molecule. It is most likely a critical structural element for dua

SUBMITTER: Szczepanska K 

PROVIDER: S-EPMC8739840 | biostudies-literature | 2022 Jan

REPOSITORIES: biostudies-literature