A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity
| Autor: | Tetsuji Noguchi, Yuki Domon, Koichi Yabe, Teppei Fujimoto, Rieko Takano, Yumi Kawase, Kazufumi Kubota, Umezaki Yuma, Miki Yokoyama, Kousei Shimada, Kenjiro Ueda |
|---|---|
| Rok vydání: | 2021 |
| Předmět: |
Clinical Biochemistry
Oliceridine Analgesic Pain Pharmaceutical Science Mice Inbred Strains (+)-Naloxone Pharmacology 01 natural sciences Biochemistry Fentanyl Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Animals Amines Molecular Biology Acetic Acid Pain Measurement Analgesics Dose-Response Relationship Drug Molecular Structure Bicyclic molecule 010405 organic chemistry Organic Chemistry Bridged Bicyclo Compounds Heterocyclic 0104 chemical sciences Pethidine 010404 medicinal & biomolecular chemistry chemistry Opioid Molecular Medicine Tail flick test medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 36:127790 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2021.127790 |
| Popis: | We identified (5R)-6-methyl-5-phenyl-1,3,4,5,6,7-hexahydro-2,5-methano-2,6-benzodiazonine (DS21980956: 4-(R)) as a novel [5.2.1]bicyclic basic compound. The scaffold was inspired by fentanyl or pethidine, which possess potent analgesic activities. DS21980956 had potent analgesic activity in the mouse acetic acid writhing test or tail flick test without agonistic activity at the µ opioid receptor (MOR). The mechanism of analgesic action of DS21980956 was considered to differ from a biased ligand, for example, TRV-130 (3, oliceridine). |
| Databáze: | OpenAIRE |
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