New rigid nicotine analogues are potent ligands of nicotinic receptors
Malfunctioning of nicotinic acetylcholine receptors (nAChRs) is observed in various mental and neurodegenerative diseases, therefore, the search and design of nAChR ligands is of particular interest. Researchers from the Department of Molecular Neuroimmune Signalling of IBCH, Russian Academy of Sciences in collaboration with colleagues from the University of Florence (Italy) designed new nicotine analogues and revealed their high affinity for α4β2 and α7 nAChRs using radioligand binding assay. In the electrophysiological and calcium imaging experiments some selected compounds showed α7 and α3β2 agonistic properties, while on the α4β2, compounds 1a and 2a behaved as antagonists. Results of the study are published in Journal of Medicinal Chemistry.