A novel calcium-sensing receptor antagonist transiently stimulates parathyroid hormone secretion in vivo

Endocrinology

Volumn 146, Issue 4, 2005, Pages 2015-2022

  Arey, Brian J ^a   Seethala, Ramakrishna ^a   Ma, Zhengping ^a   Fura, Aberra ^a   Morin, Jennifer ^a   Swartz, JoAnn ^a   Vyas, Viral ^a   Yang, Wu ^a   Dickson Jr , John K ^a   Feyen, Jean H M ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 CHLORO 6 [3 [1,1 DIMETHYL 2 (2 NAPHTHYL)ETHYLAMINO] 2 HYDROXYPROPOXY]BENZONITRILE; CALCIUM; CALCIUM SENSING RECEPTOR; CALCIUM SENSING RECEPTOR ANTAGONIST; G PROTEIN COUPLED RECEPTOR; INOSITOL PHOSPHATE; RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL EXPERIMENT; ARTICLE; BONE METABOLISM; CALCIUM HOMEOSTASIS; CALCIUM TRANSPORT; CONTROLLED STUDY; DRUG HALF LIFE; DRUG STRUCTURE; HUMAN; HUMAN CELL; IC 50; KIDNEY; MALE; NONHUMAN; OSTEOPOROSIS; PARATHYROID GLAND; PARATHYROID HORMONE BLOOD LEVEL; PARATHYROID HORMONE RELEASE; PRIORITY JOURNAL; RAT;

ANIMALS; CALCIUM; DOSE-RESPONSE RELATIONSHIP, DRUG; MALE; NAPHTHALENES; OSTEOPOROSIS; PARATHYROID HORMONE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, CALCIUM-SENSING;

EID: 20144382860     PISSN: 00137227     EISSN: None     Source Type: Journal    
DOI: 10.1210/en.2004-1318     Document Type: Article

References (27)

1. Yamaguchi T, Olozak I, Chattopadhyay N, Butters RR, Kifor O, Scadden DT, Brown EM 1998 Expression of extracellular calcium (Ca2+o)-sensing receptor in human peripheral blood monocytes. Biochem Biophys Res Commun 246: 501-506
2. i signaling expressed by GCT23 osteoclast-like cells. Proc Assoc Am Physicians 111:70-81
3. o)-sensing receptor in the clonal osteoblast-like cell lines, UMR-106 and SAOS-2. Biochem Biophys Res Commun 243:753-757
4. Godwin SL, Soltoff SP 2002 Calcium-sensing receptor-mediated activation of phospholipase C-γ1 is downstream of phospholipase C-β and protein kinase C in MC3T3-E1 osteoblasts. Bone 30:559-566
5. Hofer AM, Brown EM 2003 Extracellular calcium sensing and signalling. Nat Rev Mol Cell Biol 4:530-538
6. 2+ concentrations on the levels of inositol 1,3,4,5-tetrakisphosphate in bovine parathyroid cells. Endocrinology 124:838-844
7. 2+-sensing receptor from bovine parathyroid. Nature 366:575-580
8. 2+-sensing receptor from parathyroid and kidney: new insights into the physiology and pathophysiology of calcium metabolism. Nephrol Dial Transplant 9:1703-1706
9. Garrett JE, Capuano IV, Hammerland LG, Hung BC, Brown EM, Hebert SC, Nemeth EF, Fuller F 1995 Molecular cloning and functional expression of human parathyroid calcium receptor cDNAs. J Biol Chem 270:12919-12925
10. Brown EM, MacLeod RJ 2001 Extracellular calcium sensing and extracellular calcium signaling. Physiol Rev 81:239-297
11. o-sensing receptor. J Biol Chem 271:19537-19545
12. Dempster DW, Cosman F, Parisien M, Shen V, Lindsay R 1993 Anabolic actions of parathyroid hormone. Endocr Rev 14:690-709
13. Kimmel DB, Bozzato RP, Kronis KA, Coble T, Sindrey D, Kwong P, Recker RR 1993 The effect of recombinant human (1-84) or synthetic (1-34) parathyroid hormone on the skeleton of adult ovariectomized rats. Endocrinology 132:1577-1584
14. Nemeth EF 2002 Pharmacological regulation of parathyroid hormone secretion. Curr Pharm Des 8:2077-2087
15. 2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther 299:323-331
16. Gowen M, Stroup GB, Dodds RA, James IE, Votta BJ, Smith BR, Bhatnagar PK, Lago AM, Callahan JF, DelMar EG, Miller MA, Nemeth EF, Fox J 2000 Antagonizing the parathyroid calcium receptor stimulates parathyroid hormone secretion and bone formation in osteopenic rats. J Clin Invest 105:1595-1604
17. Arey BJ, Stevis PE, Deecher DC, Shen ES, Frail DE, Negro-Vilar A, Lopez FJ1997 Induction of promiscuous G protein coupling of the follicle-stimulating hormone (FSH) receptor: a novel mechanism for transducing pleiotropic actions of FSH isoforms. Mol Endocrinol 11:517-526
18. Nemeth EF 2002 The search for calcium receptor antagonists (calcilytics). J Mol Endocrinol 29:15-21
19. Nemeth EF, Steffey ME, Hammerland LG, Hung BC, Van Wagenen BC, DelMar EG, Balandrin MF 1998 Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proc Natl Acad Sci USA 95: 4040-4045
20. Fox J, Lowe SH, Petty BA, 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
21. 2+ and a positive allosteric modulator. J Biol Chem 277:46622-46631
22. Brauner-Osborne H, Jensen AA, Sheppard PO, O'Hara P, Krogsgaard-Larsen P 1999 The agonist-binding domain of the calcium-sensing receptor is located at the amino-terminal domain. J Biol Chem 274:18382-18386
23. 2+ receptor and on Ca2+ receptor/metabotropic glutamate chimeric receptors. Endocrinology 141:4156-4163
24. Hendy GN, D'Souza-Li L, Yang B, Canaff L, Cole DE 2000 Mutations of the calcium-sensing receptor (CASR) in familial hypocalciuric hypercalcemia, neonatal severe hyperparathyroidism, and autosomal dominant hypocalcemia. Hum Mutat 16:281-296
25. Hirai H, Nakajima S, Miyauchi A, Nishimura K, Shimizu N, Shima M, Michigami T, Ozono K, Okada S 2001 A novel activating mutation (C129S) in the calcium-sensing receptor gene in a Japanese family with autosomal dominant hypocalcemia. J Hum Genet 46:41-44
26. Jensen AA, Spalding TA, Burstein ES, Sheppard PO, O'Hara PJ, Brann MR, Krogsgaard-Larsen P, Brauner-Osborne H 2000 Functional importance of the Ala(116)-Pro(136) region in the calcium-sensing receptor. Constitutive activity and inverse agonism in a family C G-protein-coupled receptor. J Biol Chem 275:29547-29555
27. 2+ receptor. J Biol Chem 277:18908-18913