Calcium-Sensing Receptor Antagonists Small Molecules and Peptides

The calcium-sensing receptor (CaSR) is a G-protein-coupled receptor (GPCR) that senses extracellular Ca²⁺. The CaSR has wide tissue expression being found in the parathyroid gland, thyroid, kidney, intestine, skin, brain, heart, pancreas, bone and lung. First cloned from the bovine parathyroid gland in 1993, the primary role of CaSR activation is the inhibition of the release of parathyroid hormone (PTH).

CaSRs can also work independently of PTH. Local changes in extracellular Ca²⁺ regulate the ...