Correlation of lipophilicity to biodistribution of 99mTc-labelled aminothiols.
A series of 99mTc-DADT complexes substituted with heterocyclic amines were synthesized and tested for their ability to cross the BBB. Each 99mTc-DADT complex analysed by HPLC was found to consist of two epimers. The more lipophilic epimers were biodistributed in mice. The data demonstrated a significant brain uptake (3-12% dose/g whole brain) and a high lung accumulation (11-85% dose/g) at 2 min p.i. Between the partition coefficients of the technetium complexes, a linear correlation for lung accumulation was observed, while a parabolic curve for brain uptake was found.
Papadopoulos
M
M
Radiopharmaceuticals Laboratory, Institute of Radioisotopes and Radiodiagnostics, NCSR Demokritos, Attiki, Greece.
Chiotellis
E
E
Varvarigou
A
A
Mastrostamatis
S
S
Cotsyfakis
C
C
Vavouraki
H
H
Stathaki
S
S
D000818:Animals; D001812:Blood-Brain Barrier; D002851:Chromatography, High Pressure Liquid; D008055:Lipids; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D012995:Solubility; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D008055:Lipids; D015609:Organotechnetium Compounds; D013438:Sulfhydryl Compounds