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Synthesis of a novel 6,14-epoxymorphinan derivative and its pharmacology
- Source :
- Bioorganicmedicinal chemistry letters. 18(24)
- Publication Year :
- 2008
-
Abstract
- A novel 6,14-epoxymorphinan benzamide derivative (NS22) was synthesized, which showed opioid kappa receptor agonistic activity in the [(35)S]GTPgammaS binding assay. The antinociceptive effect of NS22 was evaluated in the tail-flick and the hot-plate test. This compound showed a potent antinociceptive activity in mice by s.c. administration, which was attenuated with nor-BNI (selective opioid kappa receptor antagonist).
- Subjects :
- Stereochemistry
Chemistry, Pharmaceutical
Injections, Subcutaneous
Clinical Biochemistry
Analgesic
Pharmaceutical Science
Pharmacology
Ligands
Biochemistry
Chemical synthesis
Models, Biological
Naltrexone
chemistry.chemical_compound
Mice
Drug Discovery
medicine
Animals
Benzamide
Molecular Biology
Ions
Analgesics
Chemistry
Alkaloid
Receptors, Opioid, kappa
Organic Chemistry
Antagonist
Biological activity
Hydrogen Bonding
Opioid
Models, Chemical
Morphinans
Guanosine 5'-O-(3-Thiotriphosphate)
Drug Design
Benzamides
Molecular Medicine
medicine.drug
Protein Binding
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 18
- Issue :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....d61596779c556f54ffa1b8db366f37be