Details

Autor(en) / Beteiligte

• McClure, Kim F
• Darout, Etzer
• Guimarães, Cristiano R. W
• DeNinno, Michael P
• Mascitti, Vincent
• Munchhof, Michael J
• Robinson, Ralph P
• Kohrt, Jeffrey
• Harris, Anthony R
• Moore, Dianna E
• Li, Bryan
• Samp, Lacey
• Lefker, Bruce A
• Futatsugi, Kentaro
• Kung, Daniel
• Bonin, Paul D
• Cornelius, Peter
• Wang, Ruduan
• Salter, Eben
• Hornby, Sam
• Kalgutkar, Amit S
• Chen, Yue

Titel

Activation of the G-Protein-Coupled Receptor 119: A Conformation-Based Hypothesis for Understanding Agonist Response

Ist Teil von

• Journal of medicinal chemistry, 2011-03, Vol.54 (6), p.1948-1952

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2011

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.