Read by QxMD icon Read

Edward nemeth cinacalcet

Edward F Nemeth, Bradford C Van Wagenen, Manuel F Balandrin
The extracellular calcium receptor (CaR) is a G protein-coupled receptor (GPCR) and the pivotal molecule regulating systemic Ca2+ homeostasis. The CaR was a challenging target for drug discovery because its physiological ligand is an inorganic ion (Ca2+ ) rather than a molecule so there was no structural template to guide medicinal chemistry. Nonetheless, small molecules targeting this receptor were discovered. Calcimimetics are agonists or positive allosteric modulators of the CaR, while calcilytics are antagonists and all to date are negative allosteric modulators...
2018: Progress in Medicinal Chemistry
Edward F Nemeth, Dolores Shoback
The calcium-sensing receptor (CaSR) plays a pivotal role in regulating systemic Ca(2+) homeostasis and is a target for drugs designed to treat certain disorders of bone and mineral metabolism. Calcimimetics are agonists or positive allosteric modulators of the CaSR; they inhibit parathyroid hormone (PTH) secretion and stimulate renal Ca(2+) excretion. The first calcimimetic drug is cinacalcet, a positive allosteric modulator of the CaSR that is approved for treating secondary hyperparathyroidism (HPT) in patients on renal replacement therapy and for some forms of primary HPT characterized by clinically significant hypercalcemia...
June 2013: Best Practice & Research. Clinical Endocrinology & Metabolism
Nobuo Nagano, Edward F Nemeth
Circulating levels of calcium ion (Ca(2+)) are maintained within a narrow physiological range mainly by the action of parathyroid hormone (PTH) secreted from parathyroid cells. Parathyroid cells can sense small fluctuations in plasma Ca(2+) levels by virtue of a cell surface Ca(2+) receptor (CaR) that belongs to the superfamily of G-protein-coupled receptors. Calcimimetics are positive allosteric modulators that activate the CaR on parathyroid cells and thereby immediately suppress PTH secretion. Pre-clinical studies with NPS R-568, a first generation calcimimetic compound, have demonstrated that daily oral administration inhibits the elevation of plasma PTH levels and parathyroid gland hyperplasia and ameliorates impaired bone qualities in rats with chronic renal insufficiency...
March 2005: Journal of Pharmacological Sciences
Edward F Nemeth, William H Heaton, Michael Miller, John Fox, Manuel F Balandrin, Bradford C Van Wagenen, Mathew Colloton, William Karbon, Jon Scherrer, Edward Shatzen, Gilbert Rishton, Sheila Scully, Meiying Qi, Robert Harris, David Lacey, David Martin
Calcimimetic compounds, which activate the parathyroid cell Ca(2+) receptor (CaR) and inhibit parathyroid hormone (PTH) secretion, are under experimental study as a treatment for hyperparathyroidism. This report describes the salient pharmacodynamic properties, using several test systems, of a new calcimimetic compound, cinacalcet HCl. Cinacalcet HCl increased the concentration of cytoplasmic Ca(2+) ([Ca(2+)](i)) in human embryonic kidney 293 cells expressing the human parathyroid CaR. Cinacalcet HCl (EC(50) = 51 nM) in the presence of 0...
February 2004: Journal of Pharmacology and Experimental Therapeutics
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"