| abstract |
The present invention is concerned with radiolabelled quinoline and quinolinone derivatives according Formula (I-A)* or (I-B)* showing metabotropic glutamate receptor antagonistic activity, in particular mGlu1 receptor activity, and their preparation ; it further relates to composition s comprising them, as well as their use for marking and identifying metabotrop ic glutamate receptor sites and for imaging an organ. In a preferable embodimen t, X represents O; R1 represents C1-6alkyl; cyclo3-12alkyl or (cycloC3-12alkyl) C1- 6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, hal o or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z4 - CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alky l; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula -CH2-C H2- CH2-CH2- ; R5 represents hydrogen; Y represents O; and aryl represents pheny l optionally substituted with halo. Most preferred are radiolabelled compounds in which the radioactive isotope is selected from the group of of 3H, 11C an d 18F. The invention also relates to their use in a diagnostic method, in perticular for marking and identifying a mGluR1 receptor in biological material, as well as to their use for imaging an organ, in particular using PET. |