Calindol is a phenylalkylamine calcimimetic that facilitates the activation of the calcium-sensing receptor (CaSR), a G protein-coupled receptor that triggers phosphatidylinositol (PI)-intracellular calcium signaling and, in some cell types, cell proliferation. It potently stimulates PI hydrolysis and proliferation through human CaSR (pEC50 values are 6.9 and 7.4, respectively) in the presence of calcium. Calindol directly interacts with CaSR in transmembrane domains and triggers PI hydrolysis less effectively in the absence of calcium, indicating that it is an allosteric modulator that cooperates with calcium to activate the CaSR. Calindol is used to study the properties and distribution of CaSR in different types of cells and tissues.
