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Design, synthesis and biological evaluation of novel tetrahydroisoquinoline quaternary derivatives as peripheral κ-opioid receptor agonists.
- Source :
-
Bioorganic & Medicinal Chemistry . Jul2016, Vol. 24 Issue 13, p2964-2970. 7p. - Publication Year :
- 2016
-
Abstract
- A novel series of tetrahydroisoquinoline quaternary derivatives 4 were synthesized as peripheral κ-opioid receptor agonists. All the target compounds were evaluated in κ-opioid receptor binding assays, and compounds 4l , 4m , and 4n exhibited high affinity for κ-opioid receptor. Furthermore, compound 4l (κ K i = 0.94 nM) produced potent antinociceptive activity in the mouse acetic acid-induced writhing assay, with lower sedative side effects than the parent compound MB-1c. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 09680896
- Volume :
- 24
- Issue :
- 13
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 115919864
- Full Text :
- https://doi.org/10.1016/j.bmc.2016.05.002