The effect of ligand structure on glutathione-mediated decomposition of propylene amine oxime derivatives.
Tetramethylpropyleneamine oxime (TMPAO) was synthesized and complexed to 99mTc. 99mTc-TMPAO samples, when challenged with reduced glutathione (GSH), were shown to have two GSH sensitive components, similar to a mixture of d,l and meso 99mTc-HMPAO. One component had a GSH-induced second-order dissociation rate constant (K2) similar to 99mTc-meso-HMPAO. Despite the presence of a large fraction of this component in these samples, brain uptake and autoradiographic studies with 99mTc-TMPAO were equivalent to 99mTc-d,l-HMPAO suggesting that both the d,l and meso 99mTc-TMPAO isomers are efficiently trapped in brain.
Roth
C A
CA
Research and Nuclear Medicine Services, Harry S. Truman Memorial Veterans Hospital, Columbia, MO 65211.
Hoffman
T J
TJ
Corlija
M
M
Volkert
W A
WA
Holmes
R A
RA
D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism*; D005978:Glutathione / Q000494:pharmacology*; D007536:Isomerism; D007700:Kinetics; D008297:Male; D015609:Organotechnetium Compounds / Q000378:metabolism* / Q000493:pharmacokinetics; D010091:Oximes / Q000378:metabolism* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D051381:Rats; D017208:Rats, Wistar; D019690:Technetium Tc 99m Exametazime; D013997:Time Factors
D015609:Organotechnetium Compounds; D010091:Oximes; D019690:Technetium Tc 99m Exametazime; D005978:Glutathione