113301-20-5Relevant articles and documents
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5
Pellicciari, Roberto,Sato, Hiroyuki,Gioiello, Antimo,Costantino, Gabriele,Macchiarulo, Antonio,Sadeghpour, Bahman M.,Giorgi, Gianluca,Schoonjans, Kristina,Auwerx, Johan
, p. 4265 - 4268 (2007)
23-Alkyl-substituted and 6,23-alkyl-disubstituted derivatives of chenodeoxycholic acid are identified as potent and selective agonists of TGR5, a G-protein coupled receptor for bile acids (BAs). In particular, we show that methylation at the C-23(S) position of natural BAs confers a marked selectivity for TGR5 over FXR, while the 6α-alkyl substitution increases the potency at both receptors. The present results allow for the first time a pharmacological differentiation of genomic versus nongenomic effects mediated by BA derivatives.
TGR5 MODULATORS AND METHODS OF USE THEROF
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Page/Page column 26, (2010/06/22)
The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Derivatives of biliary acids, process for the production thereof and corresponding pharmaceutical compositions
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, (2008/06/13)
New derivatives of chenodeoxycholic, ursodeoxycholic, cholic and ursocholic acids, bearing a methyl group in the side chain, in an alfa position to the carboxylic group, the corresponding nor- and di-nor- derivatives, and the corresponding conjugates with taurine and glycine, are described. The compounds of the invention are prepared by methylation of the esters with methyl iodide in the presence of lithium-dialkylamides.