Physiological and pharmacological agonists of the extracellular Ca2+-sensing receptor.
Extracellular Ca(2+) concentration [Ca(2+)](o) is vital for a number of processes varying from blood clotting to regulation membrane permeability and excitability. For this reason [Ca(2+)](o) is under strict control of a complex homeostatic system that includes parathyroid glands, kidneys, bones and intestine. The extracellular Ca(2+)-sensing receptor is an essential component of this system, regulating parathyroid hormone secretion, Ca(2+) (and Mg(2+)) excretion by the kidney, bone remodeling and Ca(2+) reabsorption by the gastrointestinal tract. The Ca(2+)-sensing receptor is also present in organs without an obvious link with mineral ion metabolism. This review will describe the discovery of a novel class of ion-sensing receptor(s), receptor-effector coupling and the roles of the Ca(2+)-sensing receptor inside and outside the Ca(2+)(o) homeostatic system.
McLarnon
Stuart J
SJ
School of Biological Sciences, University of Manchester, G.38 Stopford Bg., Oxford Rd., Manchester M13 9PT, UK.
Riccardi
Daniela
D
D000814:Aniline Compounds / Q000627:therapeutic use; D000818:Animals; D002118:Calcium / Q000378:metabolism; D006801:Humans; D008274:Magnesium / Q000378:metabolism; D009994:Osmolar Concentration; D010627:Phenethylamines; D011437:Propylamines; D044169:Receptors, Calcium-Sensing / Q000819:agonists / Q000187:drug effects / Q000502:physiology*
D000814:Aniline Compounds; C107873:N-(2-chlorophenylpropyl)-1-(3-methoxyphenyl)ethylamine; C111654:NPS R-467; D010627:Phenethylamines; D011437:Propylamines; D044169:Receptors, Calcium-Sensing; D008274:Magnesium; D002118:Calcium