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Bioorg Med Chem Lett. 2013 Jun 1;23(11):3175-9. doi: 10.1016/j.bmcl.2013.04.006. Epub 2013 Apr 10.

Conformational restriction in a series of GPR119 agonists: differences in pharmacology between mouse and human.

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  • 1Cardiovascular & Gastrointestinal Innovative Medicines Unit, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. jamie.scott@astrazeneca.com


A series of conformationally restricted GPR119 agonists were prepared based around a 3,8-diazabicyclo[3.2.1]octane scaffold. Examples were found to have markedly different pharmacology in mouse and human despite similar levels of binding to the receptor. This highlights the large effects on GPCR phamacology that can result from small structural changes in the ligand, together with inter-species differences between receptors.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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