| Literature DB >> 11848227 |
Susumu Sato1, Teruo Komoto, Yoshihiko Kanamaru, Noriyuki Kawamoto, Tomomi Okada, Terumitsu Kaiho, Kinichi Mogi, Shinichi Morimoto, Norimitsu Umehara, Tadayuki Koda, Akira Miyashita, Takao Sakamoto, Yasuhiro Niino, Tetsuo Oka.
Abstract
New muq-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, 12-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl]phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of delta- and kappa-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.Entities:
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Year: 2002 PMID： 11848227 DOI： 10.1248/cpb.50.292
Source DB: PubMed Journal: Chem Pharm Bull (Tokyo) ISSN： 0009-2363 Impact factor: 1.645