title: No-carrier-added (NCA) (+/-)-N-(3-[18F]fluoropropyl)-N-normetazocine-synthesis and PET studies in a baboon.
abstract: No-carrier-added (NCA) (+/-)-N-(3-[18F]Fluoropropyl)-N-normetazocine (2) was synthesized by N-alkylation of (+/-)-N-normetazocine (1) with NCA 1-[18F]fluoro-3-iodopropane in an overall radiochemical yield of 10% (EOB) with a mass of 3.5 nmol in a synthesis time of 90 min from end of bombardment (EOB). PET studies of 2 in a baboon did not indicate specificity for opiate receptor sites alone: The activity declined rapidly in the striatum, the frontal cortex and the cerebellum. The baboon total arterial plasma radioactivity clearance was very rapid and the metabolism of compound 2 in plasma was also very rapid. These results suggest that compound 2 is not a suitable radioligand for imaging opiate receptors in the human brain by positron tomography.
mesh_terms: D000818:Animals; D003496:Cyclazocine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D005260:Female; D005461:Fluorine; D007553:Isotope Labeling / Q000379:methods; D007700:Kinetics; D010215:Papio; D011868:Radioisotopes; D014055:Tomography, Emission-Computed
chemical_list: D011868:Radioisotopes; D005461:Fluorine; C047098:N-(3-fluoropropyl)-N-normetazocine; D003496:Cyclazocine