Biodistribution of lipophilic 99mTc complexes of cyclam derivatives

Several n-alkyl-cyclam derivatives were synthesized which form stable single component cationic chelates with 99mTc. These results suggest that the cyclam moiety in these derivatives complexes 99mTc in the same manner as the underivatized macrocycle. Biodistribution studies in mice show that all of these chelates are cleared from circulation by both the kidneys and liver. The ratio and rates of clearance by these organ systems is related to lipid solubility. None of the lypophilic-cationic-99mTc agents show any significant myocardial uptake. Also, these chelates show no significant ability to penetrate the blood-brain-barrier.