New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
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Manera C, Cascio MG, Benetti V, Allara M, Tuccinardi T, Martinelli A, Saccomanni G, Vivoli E, Ghelardini C, Di Marzo V, Ferrarini PL
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
Bioorg Med Chem Lett. 2007 Dec 1;17(23):6505-10. Epub 2007 Oct 1.
- PubMed ID
- 17942307 [ View in PubMed]
- Abstract
A series of new 1,8-naphthyridine and quinoline derivatives were synthesized and evaluated for their cannabinoid receptor affinity. In particular, compounds 2, 5, 11, and 13 showed a high CB(2) affinity and CB(2) versus CB(1) selectivity, in agreement with molecular modeling studies. Furthermore, compound 2 also exhibited in vivo antinociceptive effects.
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- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Rimonabant Cannabinoid receptor 1 Ki (nM) 16 N/A N/A Details