Antagonizing the parathyroid calcium receptor stimulates parathyroid hormone secretion and bone formation in osteopenic rats.

No abstract is available for this paper.

• Publication year

  2000

• Venue

  Journal of Clinical Investigation

• Publication date

  2000-06-01

• Fields of study

  Medicine

• Identifiers
  DOI 10.1172/JCI9038PMID 10841518PMCID PMC300853
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Calcium Receptors as Novel Drug Targets

  2002cited by this paper
• Parathyroid hormone 1–34 (hpth 1–34) and estrogen produce dramatic bone density increases in postmenopausal osteoporosis — results from a placebo‐controlled randomized trial

  2000influential reference
• Emerging Insights into the Role of Calcium Ions in Osteoclast Regulation

  1999cited by this paper
• Calcimimetic compound NPS R-568 stimulates calcitonin secretion but selectively targets parathyroid gland Ca(2+) receptor in rats.

  1999cited by this paper
• Development and Characterization of a Human In Vitro Resorption Assay: Demonstration of Utility Using Novel Antiresorptive Agents

  1999influential reference
• Calcimimetic Compounds: a Direct Approach to Controlling Plasma Levels of Parathyroid Hormone in Hyperparathyroidism.

  1999influential reference
• G-protein-coupled, extracellular Ca(2+)-sensing receptor: a versatile regulator of diverse cellular functions.

  1999influential reference
• Failure to Detect the Extracellular Calcium‐Sensing Receptor (CasR) in Human Osteoblast Cell Lines

  1999cited by this paper
• 21st Annual meeting of the American Society for Bone and Mineral Research. St. Louis, Missouri, USA. September 30-October 4, 1999. Abstracts.

  1999cited by this paper
• The extracellular calcium-sensing receptor: its role in health and disease.

  1998influential reference
• Disparate effects of mild, moderate, and severe secondary hyperparathyroidism on cancellous and cortical bone in rats with chronic renal insufficiency.

  1998cited by this paper
• Calcimimetics with potent and selective activity on the parathyroid calcium receptor.

  1998influential reference
• Parathyroid hormone treatment can reverse corticosteroid-induced osteoporosis. Results of a randomized controlled clinical trial.

  1998influential reference
• A calcimimetic agent acutely suppresses parathyroid hormone levels in patients with chronic renal failure. Rapid communication.

  1998influential reference
• Stimulation of calcitonin secretion by calcium receptor activators

  1998cited by this paper
• Expression of extracellular calcium (Ca2 + o)-sensing receptor in the clonal osteoblast-like cell lines, UMR-106 and SAOS-2.

  1998cited by this paper
• A randomized controlled trial to compare the efficacy of cyclical parathyroid hormone versus cyclical parathyroid hormone and sequential calcitonin to improve bone mass in postmenopausal women with osteoporosis.

  1997influential reference
• Expression of an Extracellular Calcium‐Sensing Receptor in Human and Mouse Bone Marrow Cells

  1997cited by this paper
• Medical Expenditures for the Treatment of Osteoporotic Fractures in the United States in 1995: Report from the National Osteoporosis Foundation

  1997cited by this paper
• The effects of programmed administration of human parathyroid hormone fragment (1-34) on bone histomorphometry and serum chemistry in rats.

  1997influential reference
• Short-term inhibition of parathyroid hormone secretion by a calcium-receptor agonist in patients with primary hyperparathyroidism.

  1997influential reference
• A Distinct Cation‐Sensing Mechanism in MC3T3‐E1 Osteoblasts Functionally Related to the Calcium Receptor

  1997cited by this paper
• Randomised controlled study of effect of parathyroid hormone on vertebral-bone mass and fracture incidence among postmenopausal women on oestrogen with osteoporosis.

  1997influential reference
• Plasma levels of parathyroid hormone that induce anabolic effects in bone of ovariectomized rats can be achieved by stimulation of endogenous hormone secretion.

  1997influential reference
• PTH: A future role in the management of osteoporosis?

  1996influential reference
• Human osteoclastoma‐derived stromal cells: Correlation of the ability to form mineralized nodules in vitro with formation of bone in vivo

  1996influential reference
• Quantification of the collagenolytic activity of isolated osteoclasts by enzyme‐linked immunosorbent assay

  1996influential reference
• The anabolic effect of human PTH (1-34) on bone formation is blunted when bone resorption is inhibited by the bisphosphonate tiludronate--is activated resorption a prerequisite for the in vivo effect of PTH on formation in a remodeling system?

  1995cited by this paper
• Parathyroid cell proliferation in normal and chronic renal failure rats. The effects of calcium, phosphate, and vitamin D.

  1995cited by this paper
• Agonist-receptor efficacy. I: Mechanisms of efficacy and receptor promiscuity.

  1995cited by this paper
• Parathyroid hormone monotherapy and cotherapy with antiresorptive agents restore vertebral bone mass and strength in aged ovariectomized rats.

  1995cited by this paper
• Parathyroid hormone (1-34) increases vertebral bone mass, compressive strength, and quality in old rats.

  1995influential reference
• [Epidemiology of fractures].

  1995influential reference
• The Effects of Calcium, Phosphate, and Vitamin D

  1995cited by this paper
• Increased bone mineral density after parathyroidectomy in primary hyperparathyroidism.

  1995influential reference
• Response of cortical bone to antiresorptive agents and parathyroid hormone in aged ovariectomized rats.

  1995cited by this paper
• Response of femoral neck to estrogen depletion and parathyroid hormone in aged rats.

  1995influential reference
• Molecular Cloning and Functional Expression of Human Parathyroid Calcium Receptor cDNAs (*)

  1995influential reference
• PTH has a more pronounced effect on vertebral bone mass and biomechanical competence than antiresorptive agents (estrogen and bisphosphonate)--assessed in sexually mature, ovariectomized rats.

  1994cited by this paper
• Cytokine suppressive anti-inflammatory compounds inhibit bone resorption in vitro.

  1994influential reference
• Anabolic effect of high doses of human parathyroid hormone (1–38) in mature intact female rats

  1994influential reference
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  1994cited by this paper
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  1993cited by this paper
• 15th annual meeting of the American Society for Bone and Mineral Research. Tampa, Florida, September 18-22, 1993. Abstracts.

  1993cited by this paper
• Anabolic actions of parathyroid hormone on bone.

  1993influential reference
• Cloning and characterization of an extracellular Ca2+-sensing receptor from bovine parathyroid

  1993influential reference
• Anabolic actions of parathyroid hormone on bone [published erratum appears in Endocr Rev 1994 Apr;15(2):261]

  1993cited by this paper
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  1991cited by this paper
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  1988influential reference
• Actions of recombinant human γ-interferon and tumor necrosis factor α on the proliferation and osteoblastic characteristics of human trabecular bone cells in vitro

  1988influential reference
• Actions of recombinant human gamma-interferon and tumor necrosis factor alpha on the proliferation and osteoblastic characteristics of human trabecular bone cells in vitro.

  1988cited by this paper
• Bone histomorphometry: standardization of nomenclature, symbols and units. Summary of proposed system.

  1988influential reference
• Bone histomorphometry: standardization of nomenclature, symbols, and units. Report of the ASBMR Histomorphometry Nomenclature Committee.

  1987cited by this paper
• Bone histomorphometry: Standardization of nomenclature, symbols, and units: Report of the asbmr histomorphometry nomenclature committee

  1987cited by this paper
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  1986cited by this paper
• The effects of monocyte-conditioned medium and interleukin 1 on the synthesis of collagenous and non-collagenous proteins by mouse bone and human bone cells in vitro.

  1984influential reference
• Physiological hypertrophy of the parathyroids, its cause and its relation to rickets.

  1940cited by this paper

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  2020cites this paper
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