The discovery of novel calcium sensing receptor negative allosteric modulators

Gayatri Balan,Jonathan N. Bauman,Samit Kumar Bhattacharya,Mayda Castrodad,David R. Healy,Michael Herr,Paul S. Humphries,Sandra M. Jennings,Amit S. Kalgutkar,Brendon Kapinos,Vishal Khot,Kimberly Lazarra,Mei Li,Yan Li,Constantin Neagu,Robert M. Oliver,David W. Piotrowski,David A. Price,Hong Qi,Holly A. Simmons,James A. Southers,Liuqing Wei,Yan Zhang,Vishwas M. Paralkar

The discovery of novel calcium sensing receptor negative allosteric modulators

2009

The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis.

Keywords:

Calcium-sensing receptor
Parathyroid hormone
Biochemistry
Ronacaleret
Allosteric regulation
Biological activity
Chemistry
rat model

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