N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor.
The synthesis and calcimimetic properties of N1-arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines are described. The most active compound of the series (3n, used at 10 microM) produced 97+/-11% of the maximal stimulation of [3H]IP production obtained by 10 mM Ca2+ in CHO cells expressing the calcium sensing receptor (CaSR). This calcimimetic activity was due to a specific interaction of this compound with the CaSR.
Dauban
P
P
Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette, France.
Ferry
S
S
Faure
H
H
Ruat
M
M
Dodd
R H
RH
D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism*; D006224:Cricetinae; D003959:Diamines / Q000138:chemical synthesis / Q000494:pharmacology*; D007295:Inositol Phosphates / Q000096:biosynthesis; D044169:Receptors, Calcium-Sensing; D011956:Receptors, Cell Surface / Q000187:drug effects*
D003959:Diamines; D007295:Inositol Phosphates; D044169:Receptors, Calcium-Sensing; D011956:Receptors, Cell Surface; D002118:Calcium