Katarzyna Szczepańska, Tadeusz Karcz, Maria Dichiara, Szczepan Mogilski, Justyna Kalinowska-Tłuścik, Bogusław Pilarski, Arkadiusz Leniak, Wojciech Pietruś, Sabina Podlewska, Katarzyna Popiołek-Barczyk, Laura J Humphrys, M Carmen Ruiz-Cantero, David Reiner-Link, Luisa Leitzbach, Dorota Łażewska, Steffen Pockes, Michał Górka, Adam Zmysłowski, Thierry Calmels, Enrique J Cobos, Agostino Marrazzo, Holger Stark, Andrzej J Bojarski, Emanuele Amata, Katarzyna Kieć-Kononowicz
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 (σ1 Rs). Therefore, we first focused on an in-depth analysis of the protonation states of piperazine and piperidine derivatives in the studied compounds...
July 7, 2023: Journal of Medicinal Chemistry