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. 1987;14(2):119-22.
doi: 10.1016/0883-2897(87)90141-3.

No-carrier-added (NCA) (+/-)-N-(3-[18F]fluoropropyl)-N-normetazocine-synthesis and PET studies in a baboon

C Y Shiue, R R Teng, L Q Bai, A P Wolf, C D Arnett, E J Simon

No-carrier-added (NCA) (+/-)-N-(3-[18F]fluoropropyl)-N-normetazocine-synthesis and PET studies in a baboon

C Y Shiue et al. Int J Rad Appl Instrum B. 1987.

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.

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