Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity

[Display omitted] We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic acid-induced writhing test an...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2020-11, Vol.28 (21), p.115714-115714, Article 115714
Main Authors: Arita, Tsuyoshi, Asano, Masayoshi, Kubota, Kazufumi, Domon, Yuki, Machinaga, Nobuo, Shimada, Kousei
Format: Article
Language:English
Subjects:
Alkaloid
Analgesic
Conolidine
Non-opioid analgesics
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] We identified (5′S)-10′-fluoro-6′-methyl-5′,6′-dihydro-3′H-spiro[cyclopropane-1,4′-[2,6]diaza[2,5]methano[2,6]benzodiazonin]-7′(1′H)-one, 22b (DS34942424) with a unique and original bicyclic skeleton. 22b showed an orally potent analgesic in the acetic acid-induced writhing test and formalin test in ddY mice without sedation. Moreover, 22b did not exhibit mu opioid receptor agonist activity.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2020.115714