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NPS R-467 is a **small molecule calcimimetic** developed as a selective positive allosteric modulator of the extracellular calcium-sensing receptor (CaSR), a member of the G protein-coupled receptor family[2][4][8]. By binding to an allosteric site distinct from the native calcium binding site, NPS R-467 enhances CaSR activation, which leads to increased responsiveness of the receptor to extracellular calcium[3][4][8]. Functionally, NPS R-467 has been shown to inhibit parathyroid hormone (PTH) secretion in vitro, and may have therapeutic utility in disorders of bone and mineral metabolism, such as hyperparathyroidism and osteoporosis[4]. Additionally, preclinical studies indicate that NPS R-467 protects against cadmium-induced kidney injury by restoring autophagic flux and reducing apoptosis, suggesting renoprotective potential in models of chronic kidney disease[1][5]. The compound is the R-enantiomer of NPS 467 and is significantly more active than the S-enantiomer[1][4].
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