Journal
JOURNAL OF THE SERBIAN CHEMICAL SOCIETY
Volume 85, Issue 6, Pages 711-720Publisher
SERBIAN CHEMICAL SOC
DOI: 10.2298/JSC190912118J
Keywords
piperidine; piperazine; heterobivalent; opioids; analgesics; dopaminergic
Categories
Funding
- Ministry of Education, Science and Technological Development of the Republic of Serbia [172032]
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Herein, the synthesis and pharmacological evaluation of 13 novel compounds, designed as potential heterobivalent ligands for mu-opioid receptor (MOR) and dopamine D-2 receptors (D(2)DAR), are reported. The compounds consisted of anilido piperidine and N-aryl piperazine moieties, joined by a variable-length methylene linker. The two moieties represent MOR and D(2)DAR pharmacophores, respectively. The synthesis encompassed four steps, securing the final products in 28-42 % overall yields. The approach has a considerable synthetic potential, providing access to various related structures. Pharmacological tests involved in vitro competitive assay for D(2)DAR using [H-3] spiperon, as a standard radioligand, and in vivo antinociceptive tests for MOR. The measured dopamine affinities were modest to low, while antinociceptive activity was completely absent. Therefore, the compounds of the general structure prepared in this research are unlikely to be useful as opioid-dopamine receptor heterobivalent ligands.
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