6269-68-7Relevant articles and documents
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.
Substituted 4,6-Diaminoquinolines as Inhibitors of C5a Receptor Binding
Lanza, Thomas J.,Durette, Philippe L.,Rollins, Thomas,Siciliano, Salvatore,Cianciarulo, Dana N.,et al.
, p. 252 - 258 (2007/10/02)
The anaphylatoxin C5a is implicated in a number of inflammatory diseases.It is a highly cationic protein with 13 of 74 amino acids being either arginine or lysine.A search focusing on positively charged molecules, particularly amine-containing functionali
