Calcilytic

Calcilytics are pharmaceutical drugs that act as antagonists at the calcium-sensing receptor (CaSR). This increases the secretion of parathyroid hormone (PTH), which has an anabolic effect on bone tissue, producing an increase in both bone volume and bone density. Consequently these drugs have been researched for the treatment of osteoporosis,[1][2][3] though with only limited success.[4] More recent research has suggested a number of additional applications for these drugs, such as hyperresponsiveness and inflammation in allergic asthma.[5][6][7][8]

Examples


References

  1. ↑ Nemeth EF. The search for calcium receptor antagonists (calcilytics). Journal of Molecular Endocrinology. 2002 Aug;29(1):15-21. PMID 12200226
  2. ↑ Silver J, Bushinsky D. Harnessing the parathyroids to create stronger bones. Curr Opin Nephrol Hypertens. 2004 Jul;13(4):471-6. PMID 15199299
  3. ↑ Widler L. Calcilytics: antagonists of the calcium-sensing receptor for the treatment of osteoporosis. Future Med Chem. 2011 Apr;3(5):535-47. doi: 10.4155/fmc.11.17 PMID 21526895
  4. ↑ Nemeth EF, Shoback D. Calcimimetic and calcilytic drugs for treating bone and mineral-related disorders. Best Pract Res Clin Endocrinol Metab. 2013 Jun;27(3):373-84. doi: 10.1016/j.beem.2013.02.008 PMID 23856266
  5. ↑ Kim JY, Ho H, Kim N, Liu J, Tu CL, Yenari MA, Chang W. Calcium-sensing receptor (CaSR) as a novel target for ischemic neuroprotection. Ann Clin Transl Neurol. 2014 Nov;1(11):851-66. doi: 10.1002/acn3.118 PMID 25540800
  6. ↑ Aggarwal A, Prinz-Wohlgenannt M, Tennakoon S, Höbaus J, Boudot C, Mentaverri R, Brown EM, Baumgartner-Parzer S, Kállay E. The calcium-sensing receptor: A promising target for prevention of colorectal cancer. Biochim Biophys Acta. 2015 Feb 18. pii: S0167-4889(15)00051-8. doi: 10.1016/j.bbamcr.2015.02.011 PMID 25701758
  7. ↑ Dal Prà I, Chiarini A, Armato U. Antagonizing amyloid-β/calcium-sensing receptor signaling in human astrocytes and neurons: a key to halt Alzheimer's disease progression? Neural Regen Res. 2015 Feb;10(2):213-8. doi: 10.4103/1673-5374.152373 PMID 25883618
  8. ↑ Yarova PF, et al. Calcium-sensing receptor antagonists abrogate airway hyperresponsiveness and inflammation in allergic asthma. Science Translational Medicine 22 April 2015;7(284):284ra60 doi: 10.1126/scitranslmed.aaa0282
  9. 1 2 3 Letz, S; et al. (2014), "Amino alcohol- (NPS-2143) and quinazolinone-derived calcilytics (ATF936 and AXT914) differentially mitigate excessive signalling of calcium-sensing receptor mutants causing Bartter syndrome Type 5 and autosomal dominant hypocalcemia", PLoS One, 9 (12): e115178, doi:10.1371/journal.pone.0115178, PMC 4266668Freely accessible, PMID 25506941.
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