916072-97-4Relevant academic research and scientific papers
Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects
Inagaki, Masanao,Kume, Masaharu,Tamura, Yoshinori,Hara, Shinichiro,Goto, Yoshihisa,Haga, Nobuhiro,Hasegawa, Tsuyoshi,Nakamura, Takashi,Koike, Katsumi,Oonishi, Shuuichi,Kanemasa, Toshiyuki,Kai, Hiroyuki
, p. 73 - 77 (2019)
Structure-activity relationship studies of several morphinan derivatives were conducted to obtain dual antagonists for μ- and δ-opioid receptors. We discovered peripherally restricted dual antagonists for μ/δ-opioid receptors as a new chemotype with a morphinan scaffold, which are orally available and do not easily pass the blood–brain barrier. As we expected, some of these compounds inhibit opioid-induced constipation and emesis/vomiting with limited potential to interfere the analgesic effects of morphine. Among them, naldemedine was selected as a potential drug candidate.
