Literature DB >> 17177896

Synthesis and in vitro evaluation of novel 2-oxo-1,2-dihydroquinoline CB2 receptor inverse agonists.

Katri H Raitio1, Juha R Savinainen, Tapio Nevalainen, Tomi Järvinen, Jouko Vepsäläinen.   

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]GTPgammaS membrane-binding assay. Compounds 7-18 produced CB2 inverse agonist activities with a variety of potencies (IC50: 1 nm-1 microm). By contrast, no considerable antagonism of CB1 receptor was observed by 1-10 microm concentrations indicating that synthesized compounds were CB2 receptor selective.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 17177896     DOI: 10.1111/j.1747-0285.2006.00452.x

Source DB:  PubMed          Journal:  Chem Biol Drug Des        ISSN: 1747-0277            Impact factor:   2.817


  2 in total

1.  Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives.

Authors:  Nashaat Turkman; Aleksander Shavrin; Roman A Ivanov; Brian Rabinovich; Andrei Volgin; Juri G Gelovani; Mian M Alauddin
Journal:  Bioorg Med Chem       Date:  2011-08-05       Impact factor: 3.641

2.  Whole-body biodistribution and radiation dosimetry of the cannabinoid type 2 receptor ligand [11C]-NE40 in healthy subjects.

Authors:  Rawaha Ahmad; Michel Koole; Nele Evens; Kim Serdons; Alfons Verbruggen; Guy Bormans; Koen Van Laere
Journal:  Mol Imaging Biol       Date:  2013-08       Impact factor: 3.488

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.