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The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core

โœ Scribed by Paul E. Harrington; David J. St. Jean Jr.; Jeffrey Clarine; Thomas S. Coulter; Michael Croghan; Adam Davenport; James Davis; Chiara Ghiron; Jonathan Hutchinson; Michael G. Kelly; Fred Lott; Jenny Ying-Lin Lu; David Martin; Sean Morony; Steve F. Poon; Elena Portero-Larragueta; Jeff D. Reagan; Kelly A. Regal; Andrew Tasker; Minghan Wang; Yuhua Yang; Guomin Yao; Qingping Zeng; Charles Henley III; Christopher Fotsch


Book ID
104004665
Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
639 KB
Volume
20
Category
Article
ISSN
0960-894X

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โœฆ Synopsis


The discovery of a series of novel and orally efficacious type II calcimimetics, developed from the lead compound 1, is described herein. Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model.


๐Ÿ“œ SIMILAR VOLUMES


An orally bioavailable positive alloster
โœ Stephen P. East; Samantha Bamford; Matthias G.A. Dietz; Christian Eickmeier; Ada ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 616 KB

A high-throughput screening campaign identified 4-((E)-styryl)-pyrimidin-2-ylamine (11) as a positive allosteric modulator of the metabotropic glutamate (mGlu) receptor subtype 4. An evaluation of the structure-activity relationships (SAR) of 11 is described and the efficacy of this compound in a ha