732298-45-2Relevant academic research and scientific papers
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression
Kim, Youngjae,Tae, Jinsung,Lee, Kangho,Rhim, Hyewhon,Choo, Il Han,Cho, Heeyeong,Park, Woo-Kyu,Keum, Gyochang,Choo, Hyunah
, p. 4587 - 4596 (2014/10/15)
5-HT7 receptor (5-HT7R) is a promising target for the treatment of depression and neuropathic pain. 5-HT7R antagonists exhibited antidepressant effects, while the agonists produced strong anti-hyperalgesic effects. In our efforts to discover selective 5-HT 7R antagonists or agonists, N-biphenylylmethyl 2- methoxyphenylpiperazinylalkanamides 1 were designed, synthesized, and biologically evaluated against 5-HT7R. Among the synthesized compounds, N-2′-chlorobiphenylylmethyl 2- methoxyphenylpiperazinylpentanamide 1-8 showed the best binding affinity with a Ki value of 8.69 nM and it was verified as a novel antagonist according to functional assays. The compound 1-8 was very selective over 5-HT1DR, 5-HT2AR, 5-HT3R, 5-HT5AR and 5-HT6R and moderately selective over 5-HT1AR, 5-HT1BR and 5-HT2CR. The novel 5-HT7R antagonist 1-8 exhibited an antidepressant effect at a dose of 25 mg/kg in the forced swimming test in mice and showed a U-shaped dose-response curve which typically appears in 5-HT7R antagonists such as SB-269970 and lurasidone.
COMPSITIONS, SYNTHESIS, AND METHODS OF USING QUINOLINE BASED ATYPICAL ANTIPSYCHOTIC AGENTS
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Page/Page column 26-27, (2009/01/20)
The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.
Novel quinazolinone derivatives as 5-HT7 receptor ligands
Na, Yong Ho,Hong, Sung Ho,Lee, Jung Hyang,Park, Woo-Kyu,Baek, Du-Jong,Koh, Hun Yeong,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
, p. 2570 - 2578 (2008/09/21)
5-HT7 receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT7 receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highl
