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Calcium-sensing receptor (CaSR) ligands act on the receptor that detects extracellular calcium levels. CaSR was cloned from bovine parathyroid and is a class C G protein-coupled receptor that controls parathyroid hormone secretion. Inactivating mutations in its gene cause familial hypocalciuric hypercalcemia and neonatal severe hyperparathyroidism. Calcimimetics are positive modulators that increase the receptor's sensitivity to calcium; examples here are cinacalcet, evocalcet and tecalcet hydrochloride. Calcilytics such as NPS-2143 and SB-423557 act in the opposite way and are used to study parathyroid and kidney calcium handling.
Calindol hydrochloride is a positive allosteric modulator (PAM) of the calcium-sensing receptor (CaSR), acting as a calcimimetic compound. It enhances CaSR activation with an EC50 of 132 nM, making it a valuable tool for studying calcium homeostasis and related signaling pathways.
Calhex 231 hydrochloride is a potent negative allosteric modulator of the calcium-sensing receptor (CaSR), with an IC50 of 0.39 μM for inhibiting \[³H]inositol phosphate accumulation induced by CaSR activation. It transiently blocks signaling through the human wild-type CaSR and is utilized in research related to traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM), where dysregulated calcium signaling contributes to disease pathology.
Calhex 231 is a potent negative allosteric modulator targeting the calcium-sensing receptor (CaSR), exhibiting an IC50 of 0.39 μM for inhibiting increases in [3H]inositol phosphates. This compound is instrumental in research applications related to traumatic hemorrhagic shock and diabetic cardiomyopathy, providing insights into the roles of CaSR in these pathophysiological conditions. Calhex 231 offers a valuable tool for investigating the modulation of CaSR signaling pathways.
