A novel class of Tc-99m complexes able to cross the blood brain barrier has been investigated and described here. These compounds are formed by reacting the bis-substituted nitrido precusors [Tc-99m(N)(PS)(2)] (PS = phosphinothiol ligand) with triethylborane (BEt3) under strictly anhydrous conditions and using non-aqueous solvents. The molecular structure of these tracers was not fully established, but preliminary experimental evidence suggests that they result from the interaction of the Lewis base [99mTc(N)(PS) 2] with the Lewis acid BEt3, which leads to the formation of the novel-B-N Tc-adduct. After purification and recovery in a physiological solution, the new boranenitrido Tc-99m derivatives were injected in rats for evaluating their in vivo biological behavior. Results showed a significant accumulation in brain tissue, thus indicating that these complexes are capable of penetrating the intact blood brain barrier. Uptake in the central nervous system was confirmed by imaging the distribution of activity on the integrated living animal using a YAP(S) SPECT small animal scanner.
Novel Tc-99m radiotracer for brain imaging
BOSCHI, Alessandra;PASQUALI, Micol;UCCELLI, Licia;DUATTI, Adriano
2007
Abstract
A novel class of Tc-99m complexes able to cross the blood brain barrier has been investigated and described here. These compounds are formed by reacting the bis-substituted nitrido precusors [Tc-99m(N)(PS)(2)] (PS = phosphinothiol ligand) with triethylborane (BEt3) under strictly anhydrous conditions and using non-aqueous solvents. The molecular structure of these tracers was not fully established, but preliminary experimental evidence suggests that they result from the interaction of the Lewis base [99mTc(N)(PS) 2] with the Lewis acid BEt3, which leads to the formation of the novel-B-N Tc-adduct. After purification and recovery in a physiological solution, the new boranenitrido Tc-99m derivatives were injected in rats for evaluating their in vivo biological behavior. Results showed a significant accumulation in brain tissue, thus indicating that these complexes are capable of penetrating the intact blood brain barrier. Uptake in the central nervous system was confirmed by imaging the distribution of activity on the integrated living animal using a YAP(S) SPECT small animal scanner.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
