Abstract

Functionalisation of an L-RNA oligonucleotide with 1,4,7,10-tetraazacyclododecane-N,N,N,N- tetraacetic acid (DOTA) was performed using the N-succinimide ester 2. The DOTA-functionalised L-RNA oligonucleotide 3 was radiolabelled with the positron-emitting radiometals 86Y(III) and 68Ga(III) in radiochemical yields of 76% and 93%, respectively. Compound 4a represents the first example of an oligonucleotide labelled with the positron emitter 86 Y. Biodistribution studies of the 86Y-radiolabelled L-RNA oligonucleotide 4a were performed in Wistar rats showing higher levels of radioactivity in the adrenal glands and kidneys. The low bone uptake (0.19%ID/g after 60 min) is indicative of the high kinetic stability of the 86Y-DOTA chelate in vivo.

Keywords: 86Y, 68Ga, DOTA, L-RNA oligonucleotide, positron emission tomography (PET)