@article{WaelbroeckCamusTastenoyetal.1994,
  author    = {Waelbroeck, M. and Camus, J. and Tastenoy, M. and Feifel, R. and Mutschler, E. and Tacke, R. and Strohmann, C. and Rafeiner, K. and Rodrigues de Miranda, J. F. and Lambrecht, G.},
  title     = {Binding and functional properties of hexocyclium and sila-hexocyclium derivatives to muscarinic receptor suhtypes},
  series = {British Journal of Pharmacology},
  volume    = {112},
  journal   = {British Journal of Pharmacology},
  url       = {http://nbn-resolving.de/urn:nbn:de:bvb:20-opus-128265},
  pages     = {505-514},
  year      = {1994},
  abstract  = {1 We have compared the binding properties of several hexocyclium and sila-hexocyclium derivatives to muscarinic Ml receptors (in rat brain, human neuroblastoma (NB-OK I) cells and calf superior cervical ganglia), rat heart M2 receptors, rat pancreas M3 receptors and M4 receptors in rat striatum, with their functional antimuscarinic properties in rabbit vas deferens (Ml/M4-like), guinea-pig atria (M2), and guinea-pig ileum (M3) muscarinic receptors. 2 Si la-substitution (C/Si exchange) of hexocyclium (~ sila-hexocyclium) and demethyl-hexocyclium (~demethyl-sila-hexocyclium) did not significantly affect their affinities for muscarinic receptors. By contrast, sila-substitution of demethoxy-hexocyclium increased its affinity 2 to 3 fold for all the muscarinic receptor subtypes studied. 3 The p-fluoro- and p-chloro-derivatives of sila-hexocyclium had lower affinities than the parent compound at the four receptor subtypes, in binding and pharmacological studies. 4 In binding studies, o-methoxy-sila-hexocyclium (Ml = M4 ~ M3 ~ M2) had a much lower affinity than sila-hexocyclium for the four receptor subtypes, and discriminated the receptor subtypes more poorly than sila-hexocyclium (Ml = M3> M4> M2)' This is in marked contrast with the very clear selectivity of demethoxy-sila-hexocyclium for the prejunctional MtlM4-like heteroreceptors in rabbit vas deferens. 5 The tertiary amines demethyl-hexocyclium, demethyl-sila-hexocyclium and demethyl-o-methoxy-silahexocyclium had 10 to 30 fold lower affinities than the corresponding quaternary ammonium derivatives.},
  language  = {en}
}