nps2143 has been researched along with Osteoporosis* in 5 studies
1 review(s) available for nps2143 and Osteoporosis
| Article | Year |
|---|---|
Emerging targets in osteoporosis disease modification.
Topics: Animals; Biomarkers; Bone Density; Bone Resorption; Humans; Osteoporosis | 2010 |
4 other study(ies) available for nps2143 and Osteoporosis
| Article | Year |
|---|---|
New aminopropandiol derivatives as orally available and short-acting calcium-sensing receptor antagonists.
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. Topics: Animals; Biological Availability; Osteoporosis; Parathyroid Hormone; Propanolamines; Rats; Receptors, Calcium-Sensing; Structure-Activity Relationship | 2010 |
The discovery of novel calcium sensing receptor negative allosteric modulators.
The design and profile of a series of zwitterionic calcium sensing receptor negative allosteric modulators is described. Evaluation of key analogues using a rat model demonstrate a robust response, significantly improved potency over ronacaleret and have the potential as an oral, anabolic treatment for osteoporosis. Topics: Administration, Oral; Allosteric Regulation; Anabolic Agents; Animals; Cell Line; Cyclopropanes; Drug Discovery; Humans; Indans; Microsomes, Liver; Osteoporosis; Phenylpropionates; Rats; Receptors, Calcium-Sensing | 2009 |
3H-Quinazolin-4-ones as a new calcilytic template for the potential treatment of osteoporosis.
Structure-activity relationship studies, focused on identification of the active pharmacophore fragments in a single high-throughput screening calcilytic hit, resulted in the discovery of potent calcium receptor antagonists, substituted 3H-quinazolin-4-ones. Topics: Animals; Male; Models, Chemical; Molecular Structure; Osteoporosis; Parathyroid Hormone; Quinazolines; Rats; Rats, Sprague-Dawley; Receptors, Calcium-Sensing; Structure-Activity Relationship | 2005 |
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.
A 3D quantitative structure-activity relationship study for inhibition of calcium-sensing receptor in the aryloxypropanolamine series predicted that these molecules adopt a U-shaped conformation with pi-stacking between the two aromatic rings. This hypothesis led to the discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines capable of antagonizing the calcium-sensing receptor with potency comparable to that of NPS-2143. Topics: Ethanolamines; Humans; Models, Molecular; Molecular Conformation; Osteoporosis; Protein Conformation; Pyrrolidines; Receptors, Calcium-Sensing; Structure-Activity Relationship | 2005 |