scholarly journals Synthesis and in Vitro and in Vivo Pharmacological Evaluation of New 4-Aminoquinoline-Based Compounds

2013 ◽  
Vol 4 (12) ◽  
pp. 1198-1202 ◽  
Author(s):  
Matshawandile Tukulula ◽  
Mathew Njoroge ◽  
Efrem T. Abay ◽  
Grace C. Mugumbate ◽  
Lubbe Wiesner ◽  
...  
Keyword(s):  
Pharmacological Evaluation

scholarly journals In vitro and in vivo pharmacological evaluation of the synthetic cannabinoid receptor agonist EG-018

2020 ◽  
Vol 193 ◽  
pp. 172918
Author(s):  
Thomas F. Gamage ◽  
Daniel G. Barrus ◽  
Richard C. Kevin ◽  
David B. Finlay ◽  
Timothy W. Lefever ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Cannabinoid Receptor ◽  
Synthetic Cannabinoid ◽  
Pharmacological Evaluation ◽  
Synthetic Cannabinoid Receptor Agonist

Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-1-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents

2012 ◽  
Vol 22 (4) ◽  
pp. 1660-1673 ◽  
Author(s):  
Kondapalli Venkata Gowri Chandra Sekhar ◽  
Vajja Sambasiva Rao ◽  
Winnie Deuther-Conrad ◽  
Divya Sridhar ◽  
Hunsur Nagendra Nagesh ◽  
...  
Keyword(s):  
Atypical Antipsychotic ◽  
Antipsychotic Agents ◽  
Design Synthesis ◽  
Pharmacological Evaluation ◽  
Atypical Antipsychotic Agents

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

2020 ◽  
Vol 85 (6) ◽  
pp. 711-720
Author(s):  
Ivana Jevtic ◽  
Jelena Penjisevic ◽  
Katarina Savic-Vujovic ◽  
Dragana Srebro ◽  
Sonja Vuckovic ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Opioid Receptor ◽  
General Structure ◽  
D2 Receptors ◽  
Antinociceptive Activity ◽  
D2 Dopamine Receptor ◽  
Pharmacological Evaluation ◽  
Pharmacological Tests

Herein, the synthesis and pharmacological evaluation of 13 novel compounds, designed as potential heterobivalent ligands for ?-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 ligands.

MF-8, a novel promising arylpiperazine-hydantoin based 5-HT 7 receptor antagonist: In vitro drug-likeness studies and in vivo pharmacological evaluation

2018 ◽  
Vol 28 (5) ◽  
pp. 878-883 ◽  
Author(s):  
Gniewomir Latacz ◽  
Annamaria Lubelska ◽  
Magdalena Jastrzębska-Więsek ◽  
Anna Partyka ◽  
Katarzyna Kucwaj-Brysz ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Pharmacological Evaluation
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