@misc{10481/83913,
year = {2023},
month = {7},
url = {https://hdl.handle.net/10481/83913},
abstract = {In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series of compounds structurally
based on highly active in vivo ligands previously studied and described by our team. However, we kept in mind that within the
previous series, a pair of closely related compounds, KSK67 and KSK68, differing only in the piperazine/piperidine moiety in the
structural core showed a significantly different affinity at sigma-1 receptors (σ1Rs). Therefore, we first focused on an in-depth
analysis of the protonation states of piperazine and piperidine derivatives in the studied compounds. In a series of 16 new ligands,
mainly based on the piperidine core, we selected three lead structures (3, 7, and 12) for further biological evaluation. Compound 12
showed a broad spectrum of analgesic activity in both nociceptive and neuropathic pain models based on the novel molecular
mechanism.},
publisher = {ACS Publications},
title = {Dual Piperidine-Based Histamine H3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain},
doi = {10.1021/acs.jmedchem.3c00430},
author = {Szczepanska, Katarzyna and Ruiz Cantero, María del Carmen and Cobos del Moral, Enrique José},
}