60987-18-0Relevant academic research and scientific papers
Ligands for the common allosteric site of acetylcholine M2-receptors: Development and application
Holzgrabe,Bender,Botero Cid,Staudt,Pick,Pfletschinger,Balatkova,Traenkle,Mohr
, p. 149 - 155 (2000)
Ligands for the allosteric site of acetylcholine M2 receptors are able to retard the dissociation of simultaneously bound ligands for the orthosteric site. This effect promotes receptor occupation by the orthosteric ligand. The allosteric effec
Structure-activity relationships in a series of bisquaternary bisphthalimidine derivatives modulating the muscarinic M2-receptor allosterically
Botero Cid, Hector M.,Tr?nkle, Christian,Baumann, Knut,Pick, Rainer,Mies-Klomfass, Elisabeth,Kostenis, Evi,Mohr, Klaus,Holzgrabe, Ulrike
, p. 2155 - 2164 (2007/10/03)
Hexane-bisammonium-type compounds containing lateral phthalimide moieties are well-established ligands of the common allosteric binding site of muscarinic M2 receptors. Previous structure-activity relationships (SAR) revealed two positively charged centers and two lateral phthalimide moieties in a defined arrangement to be essential of a high allosteric potency. The purpose of this study was to replace one carbonyl group of the phthalimides with hydrogens, hydroxy, alkoxy, phenyl, benzyl, and benzylidene groups in order to check the influence of these substituents on the allosteric activity in antagonist-linked receptors. The analysis of the quantitative SAR indicated that a high allosteric potency is related to a certain amount of rigidity as well as polarizibility and the ability to form hydrophobic interactions.
