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μ-opioid/D2 dopamine receptor pharmacophore containing ligands: Synthesis and pharmacological evaluation

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2020
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Authors
Jevtić, Ivana I.
Penjišević, Jelena
Savić-Vujović, Katarina
Srebro, Dragana
Vučković, Sonja M.
Ivanović, Milovan
Kostić-Rajačić, Slađana
Article (Published version)
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Abstract
Herein, the synthesis and pharmacological evaluation of 13 novel compounds, designed as potential heterobivalent ligands for μ-opioid receptor (MOR) and dopamine D2 receptors (D2DAR), 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 D2DAR 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 D2DAR using [3H] 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 li...gands.

Keywords:
piperidine / piperazine / heterobivalent / opioids / analgesics / dopaminergic
Source:
Journal of the Serbian Chemical Society, 2020, 85, 6, 711-720
Publisher:
  • Serbian Chemical Society
Projects:
  • Structure-activity relationship of newly synthesized biological active compound (RS-172032)

DOI: 10.2298/JSC190912118J

ISSN: 0352-5139

WoS: 000548146900002

Scopus: 2-s2.0-85090445912
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URI
http://cherry.chem.bg.ac.rs/handle/123456789/4243
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