79669-48-0Relevant academic research and scientific papers
OXEPIN DERIVATIVE
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, (2009/06/27)
The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic actio
4-Aminoquinolines: Novel nociceptin antagonists with analgesic activity
Shinkai,Ito,Iida,Kitao,Yamada,Uchida
, p. 4667 - 4677 (2007/10/03)
Small-molecule nociceptin antagonists were synthesized to examine their therapeutic potential. After a 4-aminoquinoline derivative was found to bind with the human ORL1 receptor, a series of 4-aminoquinolines and related compounds were synthesized and their binding was evaluated. Elucidation of structure - Activity relationships eventually led to the optimum compounds. One of these compounds, N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide hydrochloride (11) not only antagonized nociceptin-induced allodynia in mice but also showed analgesic effect in a hot plate test using mice and in a formalin test using rats. Its analgesic effect was not antagonized by the opioid antagonist naloxone. These results indicate that this nociceptin antagonist has the potential to become a novel type of analgesic that differs from μ-opioid agonists.
Dibenz[b,e]oxepin compounds
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, (2008/06/13)
Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
