オバタ　ヒデアキ   OBATA Hideaki   小幡　英章    所属   埼玉医科大学  医学部 総合医療センター　麻酔科（麻酔科、産科麻酔科）    職種   教授
論文種別	学術雑誌(原著)
言語種別	英語
査読の有無	査読あり
表題	In vivo and in vitro evaluation of novel mu-opioid receptor agonist compounds
掲載誌名	正式名：EUROPEAN JOURNAL OF PHARMACOLOGY ISSNコード：00142999
出版社	ELSEVIER SCIENCE BV
巻・号・頁	767,193-200頁
著者・共著者	Yoshiaki Nikaido,Aya Kurosawa,Hitomi Saikawa,Satoshi Kuroiwa,Chiharu Suzuki,Nobuo Kuwabara,Hazime Hoshino,Hideaki Obata,Shigeru Saito,Tamio Saito,Hiroyuki Osada,Isao Kobayashi,Hideki Sezutsu,Shigeki Takeda
発行年月	2015/11
概要	Opioids are the most effective and widely used drugs for pain treatment. Morphine is an archetypal opioid and is an opioid receptor agonist. Unfortunately, the clinical usefulness of morphine is limited by adverse effects such as analgesic tolerance and addiction. Therefore, it is important to study the development of novel opioid agonists as part of pain control. The analgesic effects of opioids are mediated by three opioid receptors, namely opioid mu-, delta-, and kappa-receptors. They belong to the G protein-coupled receptor superfamily and are coupled to G, proteins. In the present study, we developed a ligand screening system to identify novel opioid mu-receptor agonists that measures [S-35]GTP gamma S binding to cell membrane fractions prepared from the fat body of transgenic silkworms expressing mu-receptor-G(i1)alpha fusion protein. We screened the RIKEN Natural Products Depository (NPDepo) chemical library, which contains 5848 compounds, and analogs of hit compounds. We successfully identified a novel, structurally unique compound, that we named GUM1, with agonist activity for the opioid mu-receptor (EC50 of 1.2 mu M). The Plantar Test (Hargreaves' Method) demonstrated tha
DOI	10.1016/j.ejphar.2015.10.025
PMID	26476280