作者: Edward F. Nemeth , Michael E. Steffey , John Fox
DOI: 10.1007/BF00866757
关键词: Calcium metabolism 、 Calcium-sensing receptor 、 Medicine 、 Internal medicine 、 Endocrinology 、 Calcitonin receptor 、 Parathyroid chief cell 、 Parathyroid hormone 、 Calcimimetic 、 Secondary hyperparathyroidism 、 Hyperparathyroidism
摘要: Parathyroid cells, C-cells, and certain cells in the kidney express a cell surface calcium (Ca2+) receptor which enables these to detect respond changes concentration of extracellular Ca2+. This protein is member G protein-coupled superfamily shares limited sequence homology only with metabotropic glutamate receptors. The Ca2+ primary physiological mechanism regulating secretion parathyroid hormone (PTH) plays pivotal role maintaining systemic homeostasis. Compounds that act as agonists are called calcimimetics because they mimic or potentiate effects on function. NPS R-568 small organic calcimimetic compound acts positive allosteric modulator increase sensitivity activation by In normal rats, orally administered decreases plasma levels PTH and, at higher doses, increases calcitonin. circulating two hormones explain hypocalcemia caused this compound. also effectively lowers humans rat models secondary hyperparathyroidism. Calcimimetic compounds target provide novel therapeutic approach for treating