Calcimimetic compound NPS R-568 stimulates calcitonin secretion but selectively targets parathyroid gland Ca2+ receptor in rats

Journal of Pharmacology and Experimental Therapeutics

Volumn 290, Issue 2, 1999, Pages 480-486

  Fox, John ^a   Lowe, Stacey H ^a   Conklin, Rebecca L ^a   Petty, Barbara A ^a   Nemeth, Edward F ^a  

^a NPS Pharmaceutical Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CALCIUM CHANNEL STIMULATING AGENT; CALCIUM ION; N [3 (2 CHLOROPHENYL)PROPYL] ALPHA METHYL 3 METHOXYBENZYLAMINE; PARATHYROID HORMONE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CALCIUM TRANSPORT; CONTROLLED STUDY; DOSE RESPONSE; DOSE TIME EFFECT RELATION; DRUG POTENCY; HORMONE RECEPTOR INTERACTION; HORMONE RELEASE; MALE; NONHUMAN; ORAL DRUG ADMINISTRATION; PARATHYROID GLAND; PARATHYROIDECTOMY; PRIORITY JOURNAL; RAT;

ANILINE COMPOUNDS; ANIMALS; CALCITONIN; CALCIUM; CALCIUM GLUCONATE; CALCIUM-BINDING PROTEINS; DOSE-RESPONSE RELATIONSHIP, DRUG; HYPOCALCEMIA; KINETICS; MALE; PARATHYROID GLANDS; PARATHYROIDECTOMY; RATS; RATS, SPRAGUE-DAWLEY; STIMULATION, CHEMICAL; THYROIDECTOMY;

EID: 0032763887     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (21)

1. Austin LA and Heath H III (1981) Calcitonin: Physiology and pathophysiology. N Engl J Med 304:269-278.
2. Breslau NA (1996) Calcium, magnesium and phosphorus: Renal handling and urinary excretion, in Primer on the Metabolic Bone Diseases and Disorders of Mineral Metabolism, 3rd ed. (Favus MJ ed) pp 49-57, Lippincott-Raven, Philadelphia, PA.
3. Broadus AE (1996) Mineral balance and homeostasis, in Primer on the Metabolic Bone Diseases and Disorders of Mineral Metabolism, 3rd ed. (Favus MJ ed) pp 57-63, Lippincott-Raven, Philadelphia, PA.
4. 2+ and other ions as extracellular (first) messengers. Physiol Rev 71:371-411.
5. 2+-sensing receptor from bovine parathyroid. Nature (Lond) 366:575-580.
6. Brown EM and Hebert SC (1997) Calcium-receptor-regulated parathyroid and renal function. Bone 20:303-309.
7. Deftos LJ (1996) Calcitonin, in Primer on the Metabolic Bone Diseases and Disorders of Mineral Metabolism, 3rd ed. (Favus MJ ed) pp 82-87, Lippincott-Raven, Philadelphia, PA.
8. Fox J (1988) Verapamil induces PTH resistance but increases duodenal calcium absorption in rats. Am J Physiol 255:E702-E707.
9. 3 during maturation in rats. Horm Metab Res 22:278-282.
10. Fox J, Lowe SH, Petty BA and Nemeth EF (1999) NPS R-568: A type II calcimimetic compound that acts on parathyroid cell calcium receptor of rats to reduce plasma levels of parathyroid hormone and calcium. J Pharmacol Exp Ther 290:473-479.
11. Garrett JE, Capuano IV, Hammerland LG, Hung BCP, Brown EM, Hebert SC, Nemeth EF and Fuller F (1995a) Molecular cloning and functional expression of human parathyroid calcium receptor cDNAs. J Biol Chem 270:12919-12925.
12. Garrett JE, Tamir H, Kifor O, Simin RT, Rogers KV, Mithal A, Gagel RF and Brown EM (1995b) Calcitonin-secreting cells of the thyroid express an extracellular calcium receptor gene. Endocrinology 136:5202-5211.
13. 2, and D in bovine parathyroid and CaR-transfected, human embryonic kidney (HEK293) cells. J Bone Miner Res 12:715-725.
14. 2+-sensing receptor messenger ribonucleic acid and protein. Endocrinology 136:3087-3092.
15. Nemeth EF (1990) Regulation of cytosolic calcium by extracellular divalent cations in C-cells and parathyroid cells. Cell Calcium 11:323-327.
16. Nemeth EF (1996) Calcium receptors as novel drug targets, in Principles of Bone Biology (Bilezekian JP, Raisz LG and Rodan GA eds) pp 1019-1035, Academic Press, New York.
17. Nemeth EF, Steffey ME and Fox J (1996) The parathyroid calcium receptor: A novel therapeutic target for treating hyperparathyroidism. Pediatr Nephrol 10:275-279.
18. Nemeth EF, Steffey ME, Hammerland LG, Hung BCP, Van Wagenen BC, DelMar EG and Balandrin MF (1998) Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc Natl Acad Sci USA 95:4040-4045.
19. Riccardi D, Park J, Lee W-S, Gamba G, Brown EM and Hebert SC (1995) Cloning and functional expression of a rat kidney extracellular calcium/polyvalent cation-sensing receptor. Proc Natl Acad Sci USA 92:131-135.
20. Silverberg SJ, Bone HG III, Marriott TB, Locker FG, Thys-Jacobs S, Dziem G, Kaatz S, Sanguinetti EL and Bilezekian 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.
21. + channels in the TAL. Am J Physiol 27:1:C103-C111.