Evaluation of alkylated derivatives of 99mTc-propylene amine oxime (99mTc-PnAO).
Several lipophilic di-alkylated derivatives of propylene amine oxime (PnAO were complexed to 99mTc. Assessment of the 99mTc-PnAO derivatives included biodistribution and qualitative autoradiography. All of the derivatives studied penetrated the intact blood-brain-barrier, with the 99mTc-dibutyl-PnAO complex exhibiting the lowest initial brain uptake while the 99mTc-diethyl-PnAO and the 99mTc-dipropyl-PnAO complexes possessing nearly identical initial brain uptake as compared to 99mTcPnAO. Qualitative autoradiographs revealed significant loss of image resolution with extended time post injection indicative of rapid radiopharmaceutical washout. Although increasing alkyl chain length did not enhance initial brain uptake, the data demonstrates that limited modification of the PnAO ligand structure can be performed without decreasing cerebral uptake of the respective 99mTc complex.
Hoffman
T J
TJ
Research Service, H.S. Truman Memorial Veterans Administration Hospital, Columbia, MO 65201.
Volkert
W A
WA
Corlija
M
M
McKenzie
E H
EH
Chaplin
S B
SB
Oberle
P A
PA
Holmes
R A
RA
D000818:Animals; D001345:Autoradiography; D001812:Blood-Brain Barrier / Q000187:drug effects*; D001921:Brain / Q000378:metabolism; D008297:Male; D015609:Organotechnetium Compounds / Q000493:pharmacokinetics*; D010091:Oximes / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D015609:Organotechnetium Compounds; D010091:Oximes; C044310:technetium Tc 99m propylene amine oxime