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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.
Synonyms: Mimpara; Sensipar
AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium.
Synonyms: AMG 073
AMG-073 (Cinacalcet) represents a new class of compounds for the treatment of hyperparathyroidism.
Synonyms: γ-Glu-Val
γ-Glutamylvaline (γ-Glu-Val) is a potent activator of the calcium-sensing receptor (CaSR) with demonstrated anti-inflammatory properties. This compound effectively inhibits tumor necrosis factor-alpha (TNF-α)-induced production of proinflammatory cytokines and enhances the expression of Wnt5a. Research applications for γ-Glutamylvaline include investigations into calcium-sensing receptor pathways in adipocytes, particularly in 3T3-L1 mouse models, where it has been shown to mitigate low-grade chronic inflammation.
Synonyms: Velcalcetide; AMG 416; KAI-4169
Etelcalcetide is a synthetic calcimimetic that acts as an activator of the calcium sensing receptor (CaSR). This compound effectively reduces parathyroid hormone (PTH) levels, making it a valuable tool for research in secondary hyperparathyroidism, particularly in patients undergoing hemodialysis. Its role in modulating calcium homeostasis holds potential for studying chronic kidney disease and related disorders.
