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- W2034157360 abstract "Hexane-bisammonium-type compounds containing lateral phthalimide moieties are known to have a rather high affinity for the allosteric site of muscarinic M2 receptors. In order to get more insight into the contribution of the lateral substituents for alloster binding affinity, a series of compounds with unilaterally varying imide substituents were synthesized and tested for their ability to retard allosterically the dissociation of [3H]N-methylscopolamine from the receptor protein (control t12 = 2 min; 3 mM MgHCO4, 50 mM Tris, pH 7.3, 37 °C). Among the test compounds, the naphthalimide containing agent (half maximum effect at EC50,diss = 60 nM) revealed the highest potency. Apparently, its affinity for the allosteric site in NMS-occupied receptors is 20fold higher compared with the phthalimide containing parent compound W 84. Analysis of quantitative structure-activity relationships yielded a parabolic correlation between the volume of the lateral substituents and the allosteric potency. The maximal volume was determined to be approximately 600 Å3 suggesting that the allosteric binding site contains a binding pocket of a defined size for the imide moiety." @default.
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- W2034157360 date "2000-03-01" @default.
- W2034157360 modified "2023-09-23" @default.
- W2034157360 title "Probing the size of a hydrophobic binding pocket within the allosteric site of muscarinic acetylcholine M2-receptors" @default.
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- W2034157360 doi "https://doi.org/10.1016/s0024-3205(00)00490-2" @default.
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