Calcium-Sensing Receptor Antagonists I - CAS 478963-79-0
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Not Intended for Therapeutic Use. For research use only.
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Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.
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2(1H)-Quinazolinone, 1-(1-methylethyl)-4-[4-(1-methylethyl)phenyl]-6-(2-propyn-1-yloxy)-
1.Secretory diarrhoea: mechanisms and emerging therapies.
Thiagarajah JR1, Donowitz M2, Verkman AS3. Nat Rev Gastroenterol Hepatol. 2015 Aug;12(8):446-57. doi: 10.1038/nrgastro.2015.111. Epub 2015 Jun 30.
Diarrhoeal disease remains a major health burden worldwide. Secretory diarrhoeas are caused by certain bacterial and viral infections, inflammatory processes, drugs and genetic disorders. Fluid secretion across the intestinal epithelium in secretory diarrhoeas involves multiple ion and solute transporters, as well as activation of cyclic nucleotide and Ca(2+) signalling pathways. In many secretory diarrhoeas, activation of Cl(-) channels in the apical membrane of enterocytes, including the cystic fibrosis transmembrane conductance regulator and Ca(2+)-activated Cl(-) channels, increases fluid secretion, while inhibition of Na(+) transport reduces fluid absorption. Current treatment of diarrhoea includes replacement of fluid and electrolyte losses using oral rehydration solutions, and drugs targeting intestinal motility or fluid secretion. Therapeutics in the development pipeline target intestinal ion channels and transporters, regulatory proteins and cell surface receptors.
2.[Bone and Nutrition. A prospect of calcium sensing receptor].
Endo I1. Clin Calcium. 2015 Jul;25(7):1029-36. doi: CliCa150710291036.
Following the discovery of the calcium-sensing receptor (CaSR) in 1993, its pivotal role in disorders of calcium homeostasis was demonstrated. Compelling evidence suggests that the CaSR plays multiple roles extending well beyond not only regulating the level of extracellular Ca(2+), but also controlling diverse and crucial roles in human physiology and pathophysiology. This review covers current knowledge of the role of the CaSR in disorders of calcium homeostasis (familial hypocalciuric hypercalcemia, neonatal severe hyperparathyroidism, autosomal dominant hypocalcemia, primary and secondary hyperparathyroidism, hypercalcemia of malignancy) as well as unrelated diseases such as breast and colorectal cancer, Alzheimer's disease and pancreatitis. In addition, it examines the use or potential use of CaSR agonists or antagonists in the management of disorders as diverse as hyperparathyroidism and Alzheimer's disease.
3.Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists.
Kiefer L1, Beaumard F1, Gorojankina T2, Faure H2, Ruat M2, Dodd RH3. Bioorg Med Chem. 2016 Feb 15;24(4):554-69. doi: 10.1016/j.bmc.2015.12.019. Epub 2015 Dec 12.
We report the first comprehensive structure-activity study of calindol (4, (R)-N-[(1H-indol-2-yl)methyl]-1-(1-naphthyl)ethanamine), a positive allosteric modulator, or calcimimetic, of the calcium sensing receptor (CaSR). While replacement of the naphthyl moiety of calindol by other aromatic groups (phenyl, biphenyl) was largely detrimental to calcimimetic activity, incorporation of substituents on the 4, 5 or 7 position of the indole portion of calindol was found to provide either equipotent derivatives compared to calindol (e.g., 4-phenyl, 4-hydroxy, 5-hydroxycalindol 44, 52, 53) or, in the case of 7-nitrocalindol (51), a 6-fold more active calcimimetic displaying an EC50 of 20nM. Unlike calindol, the more active CaSR calcimimetics were shown not to act as antagonists of the closely related GPRC6A receptor, suggesting a more selective profile for these new analogues.
4.Borneol inhibits TRPA1, a proinflammatory and noxious pain-sensing cation channel.
Sherkheli MA1, Schreiner B2, Haq R1, Werner M2, Hatt H2. Pak J Pharm Sci. 2015 Jul;28(4):1357-63.
Borneol, a natural product isolated from several species of Artemisia, Blumea and Kaempferia, has a widespread use in traditional medicine. TRP ion channels are a class of nonselective cation channel proteins involved in a variety of physiological and pathological processes in mammals. TRPA1, a member of TRP family of cation channels, is involved in plethora of processes including noxious-cold, noxious-pain sensations, inflammation and the detection of irritant chemicals. Borneol is chemically related to camphor (a known inhibitor of TRPA1 ion channels); therefore, it is beneficial to investigate the effects of borneol on TRPA1. In the present investigation it was found that borneol inhibits TRPA1 mediated cationic currents in low millimolar range (IC50 0.3mM) in heterologous expression systems like Xenopus oocytes and in neurons cultured from trigeminal ganglia. Effects of nicotine, a known chemical irritant and agonist of TRPA1 are also inhibited by borneol in both systems.
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CAS 478963-79-0 Calcium-Sensing Receptor Antagonists I

Calcium-Sensing Receptor Antagonists I
(CAS: 478963-79-0)

Calcium-Sensing Receptor Antagonists I is an antagonist of calcium-sensing parathyroid hormone receptors.

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CAS 478963-79-0 Calcium-Sensing Receptor Antagonists I

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