期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 5, 页码 878-883出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.02.003
关键词
5-HT7 receptor antagonist; Drug-like properties; Antidepressant-like activity; Anxiolytic-like activity; Arylpiperazines
资金
- Jagiellonian University Medical College [K/ZDS/006134, K/ZDS/005593]
- National Science Centre Poland [UMO-2014/15/N/NZ7/03072]
We report the in vitro drug-likeness studies and in vivo pharmacological evaluation for a new potent 5-HT7 receptor antagonist MF-8 (5-(4-fluorophenyl)-3-(2-hydroxy-3-(4-(2-methoxyphenyl)piperazin-1-yl) propyl)-5-methylhydantoin). The in vitro tests showed good permeability, very good metabolic stability, low risk of drug-drug interactions and satisfying safety profile. Moreover, MF-8 showed excellent antide-pressant-like activity in the forced swim test in rodents and promising anxiolytic-like activity in the fourplate test in mice. Regarding the potent affinity, high selectivity and antagonistic activity of MF-8 for the 5-HT7 receptor as well as excellent drug - like properties in vitro and confirmed in vivo pharmacological activity, MF-8 should be considered as a very significant molecule in the search for a new class of antidepressant drugs. (C) 2018 Elsevier Ltd. All rights reserved.
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