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Peer-reviewed veterinary case report

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

Journal:
Bioorganic & medicinal chemistry
Year:
2020
Authors:
Arita, Tsuyoshi et al.
Affiliation:
Medicinal Chemistry Research Laboratories · Japan
Species:
rodent

Abstract

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.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/33065431/