The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Inhibitory effects of SR141716A on G-protein activation in rat brain.

N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide hydrochloride (SR141716A), a cannabinoid CB(1) receptor antagonist, has inverse agonist effects in cannabinoid CB(1) receptor-expressing cell lines, brain and peripheral organs. These studies characterized SR141716A-inhibited G-protein activity by measuring [35S]GTPgammaS binding. Maximal inhibition of basal [35S]GTPgammaS binding in cerebellar membranes was 50%. The EC(50) value for inhibition of [35S]GTPgammaS binding was 4.4 microM, whereas the K(e) for inhibition of R(+)-[2,3-dihydro-5-methyl-3-[(morpholinyl)methyl]pyrrolo[1,2,3-de]-1,4-benzoxazinyl]-(1-naphthalenyl)methanone mesylate (WIN 55,212-2)-stimulated [35S]GTPgammaS binding was 0.6 nM. [35S]GTPgammaS autoradiography was used to examine the regional specificity of SR141716A inhibition. SR141716A inhibited basal [35S]GTPgammaS binding in all regions examined, with inhibition ranging from approximately 20% in caudate-putamen to 40% in hippocampus. These studies demonstrate that SR141716A is a competitive antagonist at nanomolar concentrations, whereas it inhibits basal receptor-mediated G-protein activity at micromolar concentrations. These data suggest that the apparent inverse agonist effect is either not cannabinoid CB(1) receptor-specific or that SR141716A is binding to different sites on the cannabinoid CB(1) receptor to produce inverse agonist versus competitive antagonist effects.[1]

References

  1. Inhibitory effects of SR141716A on G-protein activation in rat brain. Sim-Selley, L.J., Brunk, L.K., Selley, D.E. Eur. J. Pharmacol. (2001) [Pubmed]
 
WikiGenes - Universities