Synthesis and structure-activity relationship studies on a new aminopropandiol class of derivatives as calcium-sensing receptor antagonists are described. Modification of the phenolic moiety of a calcilytic compound NPS 2143 led to the identification of an orally available compound (R,R)-31 which demonstrated a rapid and transient stimulation of PTH release in rats.
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http://dx.doi.org/10.1016/j.bmcl.2010.04.035 | DOI Listing |
Theriogenology
January 2025
Robinson Research Institute, The University of Adelaide, South Australia, Australia; Discipline of Reproduction and Development, School of Biomedicine, The University of Adelaide, South Australia, Australia. Electronic address:
In vitro embryo production (IVP) is used in the cattle industry to increase the rate of genetic gain. IVP uses semen that has been frozen and thawed, a process that renders sperm less viable than sperm from fresh semen. Granulocyte macrophage colony stimulating factor (GM-CSF) is present in bovine seminal plasma, while its receptor is present on bovine sperm.
View Article and Find Full Text PDFPLoS One
January 2025
Nephrological Department, Herlev Hospital, University of Copenhagen, Copenhagen, Denmark.
Secondary hyperparathyroidism (sHPT) is a significant clinical complication of CKD leading to bone abnormalities and cardiovascular disease. Current treatment based on activating the parathyroid calcium-sensing receptor (CaSR) using calcimimetics such as Cinacalcet, aims to decrease plasma PTH levels and inhibit the progression of parathyroid hyperplasia. In the present study, we found significant diurnal rhythmicity of Casr, encoding the Cinacalcet drug target in hyperplastic parathyroid glands (p = 0.
View Article and Find Full Text PDFCurr Biol
December 2024
Department of Microbiology, Immunology, and Molecular Genetics, University of California, Los Angeles, Los Angeles, CA 90095, USA; Molecular Biology Institute, University of California, Los Angeles, Los Angeles, CA 90095, USA. Electronic address:
Skin-penetrating nematodes infect nearly one billion people worldwide. The developmentally arrested infective larvae (iL3s) seek out hosts, invade hosts via skin penetration, and resume development inside the host in a process called activation. Activated infective larvae (iL3as) traverse the host body, ending up as parasitic adults in the small intestine.
View Article and Find Full Text PDFCase Rep Endocrinol
December 2024
Henry Ford St. John Hospital, Detroit, Michigan, USA.
Front Pharmacol
December 2024
Department of Urology, The First Affiliated hospital of Gannan Medical University, Ganzhou, Jiangxi, China.
Background: The calcium-sensitive receptor (CaSR) has been identified as a key factor in the formation of kidney stones. A substantial body of research has illuminated the function of CaSR in stone formation with respect to oxidative stress, epithelial injury, crystal adhesion, and stone-associated proteins. Nevertheless, as a pivotal molecule in renal calcium excretion, its pathway that contributes to stone formation by regulating calcium supersaturation remains underexplored.
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