The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
โ 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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โฆ 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.
๐ SIMILAR VOLUMES
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