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- Title
Synthesis and In Vitro Evaluation of Novel 2-oxo-1,2-dihydroquinoline CB2 Receptor Inverse Agonists.
- Authors
Raitio, Katri H.; Savinainen, Juha R.; Nevalainen, Tapio; Järvinen, Tomi; Vepsäläinen, Jouko
- Abstract
Aliphatic amides of 7-methoxy-2-oxo-8-pentyloxy-1,2-dihydroquinoline-3-carboxylic acid 6 were synthesized and evaluated for their CB2 and CB1 receptor activities by a [35S]GTP γS membrane-binding assay. Compounds 7–18 produced CB2 inverse agonist activities with a variety of potencies (IC50: 1 nm–1 μm). By contrast, no considerable antagonism of CB1 receptor was observed by 1–10 μm concentrations indicating that synthesized compounds were CB2 receptor selective.
- Subjects
AMIDES; DRUG receptors; MICROBIOLOGICAL assay; CHEMICAL agonists; CELL receptors
- Publication
Chemical Biology & Drug Design, 2006, Vol 68, Issue 6, p334
- ISSN
1747-0277
- Publication type
Letter
- DOI
10.1111/j.1747-0285.2006.00452.x