Pharmacodynamics of the Type II Calcimimetic Compound Cinacalcet HCl

Journal of Pharmacology and Experimental Therapeutics

Volumn 308, Issue 2, 2004, Pages 627-635

  Nemeth, Edward F ^b   Heaton, William H ^b   Miller, Michael ^b   Fox, John ^b   Balandrin, Manuel F ^b   Van Wagenen, Bradford C ^b   Colloton, Mathew ^a   Karbon, William ^a   Scherrer, Jon ^a   Shatzen, Edward ^a   Rishton, Gilbert ^a   Scully, Sheila ^a   Qi, Meiying ^a   Harris, Robert ^a   Lacey, David ^a   Martin, David ^a  

^a AMGEN INC   (United States)

^b NPS Pharmaceutical Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIMIMETIC AGENT; CALCITONIN; CALCIUM; CALCIUM BINDING PROTEIN; CINACALCET; NAPHTHALENE DERIVATIVE; PARATHYROID HORMONE; PHOSPHORUS;

ANIMAL; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLOOD; CALCITONIN BLOOD LEVEL; CALCIUM BLOOD LEVEL; CALCIUM CELL LEVEL; CATTLE; CELL CULTURE; CELL STRUCTURE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; ENANTIOMER; EXTRACELLULAR CALCIUM; HUMAN; HUMAN CELL; HYPERPARATHYROIDISM; IC 50; MALE; METABOLISM; NONHUMAN; PARATHYROID GLAND; PARATHYROID HORMONE BLOOD LEVEL; PARATHYROID HORMONE RELEASE; PRIORITY JOURNAL; RAT; RAT STRAIN; STEREOCHEMISTRY;

ANIMALS; CALCITONIN; CALCIUM; CALCIUM-BINDING PROTEINS; CELLS, CULTURED; HUMANS; MALE; NAPHTHALENES; PARATHYROID GLANDS; PARATHYROID HORMONE; PHOSPHORUS; RATS; RATS, SPRAGUE-DAWLEY;

EID: 9144251958     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.103.057273     Document Type: Article

References (31)

1. Antonsen JE, Sherrard DJ, and Andress DL (1998) A calcimimetic agent acutely suppresses parathyroid hormone levels in patients with chronic renal failure. Kidney Int 53:223-227.
2. 2+-sensing receptor from bovine parathyroid. Nature (Lond) 366:575-580.
3. 2+ signaling. Physiol Rev 81:239-297.
4. Deftos LJ, Roos BA, and Oates EL (1999) Calcitonin, in Primer on the Metabolic Bone Diseases and Disorders of Mineral Metabolism, 4th ed. (Favus MJ ed) pp 99-103, Lippincott-Raven, Philadelphia, PA.
5. 2+. J Pharmacol Exp Ther 290:473-479.
6. 2+ receptor in rats. J Pharmacol Exp Ther 290:480-486.
7. Frazão JM, Martins P, and Coburn JW (2002) The calcimimetic agents: perspectives for treatment. Kidney Int 60:S149-S154.
8. Gagel RF, Zeytinoglu FN, Voelkel EF, and Tashjian AH (1980) Establishment of a calcitonin-producing rat medullary thyroid carcinoma cell line II. Secretory studies of tumor and cells in culture. Endocrinology 107:516-523.
9. 2+ receptor cDNAs. J Biol Chem 270:12919-12925.
10. 2+ receptor gene. Endocrinology 136:5202-5211.
11. 2+ x phosphorus product and parathyroid hormone with cardiac mortality risk in chronic hemodialysis patients. J Am Soc Nephrol 12:2131-2138.
12. Goodman WG, Frazão JM, Goodkin DA, Turner SA, Liu W, and Coburn JW (2000a) A calcimimetic agent lowers plasma parathyroid hormone levels in patients with secondary hyperparathyroidism. Kidney Int 58:436-445.
13. Goodman WG, Goldin, Kuizon BD, Yoon C, Gales B, Sider D, Wang Y, Chung J, Emerick A, Greaser L, et al. (2000b) Coronary-artery calcification in young adults with end-stage renal disease who are undergoing dialysis. New Engl J Med 342:1478-1483.
14. 2+ receptors. J Pharmacol Exp Ther 77:642-648.
15. 2+ receptor/metabotropic glutamate chimeric receptors. Endocrinology 141:4156-4163.
16. Kenakin T (2003) Predicting therapeutic value in the lead optimization phase of drug discovery. Nat Rev Drug Discovery 2:429-438.
17. Lavigne JR, Zahradnik RJ, Conklin RL, Lambert LD, Logan MA, Parihar A, and Fox J (1998) Stimulation of calcitonin secretion by calcium receptor activators: evaluation using a new, highly sensitive homologous immunoradiometric assay for rat calcitonin. Endocrine 9:293-301.
18. 2+ x phosphorus in secondary hyperparathyroidism. Kidney Int 63:248-254.
19. Llach F (1999) Hyperphosphatemia in end-stage renal disease patients: pathophysiological consequences. Kidney Int 56:S31-S37.
20. Nemeth EF (1996) Calcium Receptors as novel drug targets, in Principles of Bone Biology (Bilezekian, JP, LG Raisz, and GA Rodan eds) pp 1019-1035, Academic Press, San Diego, CA.
21. Nemeth EF (2002a) Pharmacological regulation of parathyroid hormone secretion. Curr Pharm Des 8:2077-2087.
22. Nemeth EF (2002b) The search for calcium receptor antagonists (calcilyties). J Mol Endocrinol 29:15-22.
23. 2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther 299:323-331.
24. Nemeth EF and Fox J (1999) Calcimimetic compounds: a direct approach to controlling plasma levels of parathyroid hormone in hyperparathyroidism. Trends Endocrinol Metab 10:66-71.
25. 2+ in bovine parathyroid cells evoked by extracellular divalent cations. J Biol Chem 262:5188-5196.
26. 2+ receptor. Proc Natl Acad Sci USA 95:4040-4045.
27. Quarles DL, Sherrard DJ, Adler S, Rosansky SJ, McCary LC, Liu W, Turner SA, and Bushinsky DA (2003) The calcimimetic AMG 073 as a potential treatment for secondary hyperparathyroidism of end-stage renal disease. J Am Soc Nephrol 14:575-583.
28. 2+ homeostasis in bovine parathyroid cells and its modulation by protein kinase-C. J Physiol (Lond) 468:141-162.
29. Racke FK and Nemeth EF (1993b) Protein kinase-C modulates hormone secretion regulated by extracellular polycations in bovine parathyroid cells. J Physiol (Lond) 468:163-176.
30. Silverberg SJ, Bone III HG, Marriott TB, Locker FG, Thysjacobs S, Dziem G, Kaatz S, Sanguinetti EL, and Bilezikian JP (1997) Short-term inhibition of parathyroid hormone secretion by a calcium-receptor agonist in patients with primary hyperparathyroidism. N Engl J Med 337:1506-1510.
31. Zeytinoglu FN, Delellis RA, Gagel RF, Wolfe HJ, and Tashjian AH (1980) Establishment of a calcitonin-producing rat medullary thyroid carcinoma cell line, I. Morphological studies of the tumor and cells in culture. Endocrinology 107:509-515.