| abstract |
The present invention relates to radiolabelled quinoline derivatives exhibiting antagonistic activity towards the metabotropic glutamate receptor, in particular activity towards the mGlu1 receptor; the invention also relates to compositions containing such derivatives, as well as their use for marking and identifying metabotropic glutamate receptor sites and for visualizing an organ. In a preferred embodiment, X is O; R is C-alkyl; cyclo-C-alkyl or (cyclo-C-alkyl) C-alkyl, where one or more hydrogen atoms in the C-alkyl group or in the cyclo-C-alkyl group may optionally be replaced by C-alkyloxy, aryl, halogen or thienyl ; Is hydrogen; halogen; C-alkyl or amino; each of R and R is independently hydrogen or C-alkyl; or R and R can be combined to form —R — R, which is a divalent radical of the formula —Z — CH — CH — CH— or —Z — CH — CH, where Z is O or NR, where R is C-alkyl; and where each divalent radical is optionally substituted with C-alkyl; or R and R may be combined to form a divalent radical of the formula —CH — CH — CH — CH — CH; Is hydrogen; Y represents O; and aryl is phenyl optionally substituted with halogen. Most preferred are radiolabelled compounds with radioactive isotopes selected from the groups H, C and F. The invention also relates to the use of such compounds in a diagnostic method, in particular for labeling and identification of the mGlu1 receptor in biological material, as well as to the use of such compounds for |