title: N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor.
abstract: 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.
authors.affiliation: Institut de Chimie des Substances Naturelles, Centre National de la Recherche Scientifique, Gif-sur-Yvette, France.
authors.forename: P
authors.initials: P
authors.lastname: Dauban
authors.forename: S
authors.initials: S
authors.lastname: Ferry
authors.forename: H
authors.initials: H
authors.lastname: Faure
authors.forename: M
authors.initials: M
authors.lastname: Ruat
authors.forename: R H
authors.initials: RH
authors.lastname: Dodd
mesh_terms: 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*
chemical_list: D003959:Diamines; D007295:Inositol Phosphates; D044169:Receptors, Calcium-Sensing; D011956:Receptors, Cell Surface; D002118:Calcium