Preparation and biological characteristics of 99mTc-diol a renal agent.
The present work concerns the production of 1,2-dihydroxypropyl-1-phosphonic acid (diol) by acid hydrolysis of (-cis) 1,2-epoxypropylphosphonic acid (phosphomycin), and its formulation as a kit easily labeled with [99mTc]pertechnetate. Biodistribution studies and whole-body autoradiographies in mice show that 99mTc-diol has a specific affinity for the kidneys: it is rapidly cleared from the blood and excreted in urine (12.09 +/- 6.40% ID are excreted in urine at 5 min and 70.81 +/- 2.41% ID at 30 min post-injection). Part of the injected activity remains in the kidney cortex sufficiently long to permit kidney imaging (5.66 +/- 0.91% ID is still in kidneys 1 h post-injection). In comparison with other agents which also localize in the kidney cortex, such as 99mTc-DMSA and 99mTc-glucoheptonate (99mTc-GHA), the main differences are the following: the peak of renal activity is reached early in the 5 min post-injection period for 99mTc-diol, only at about 10 min post-injection for 99mTc-GHA and after 3 h post-injection for 99mTc-DMSA. The uptake of 99mTc-diol by other organs, especially by bones, is much smaller than in the case of 99mTc-DMSA (1.25 +/- 0.11% ID of 99mTc-diol compared to 11.31 +/- 1.17% ID of 99mTc-DMSA, 1 h post-injection). Unlike 99mTc-DMSA, the biodistribution of 99mTc-diol is not significantly influenced by acid-base imbalance, in addition, its renal uptake decreases in the presence of probenecid whereas its urinary excretion increases.(ABSTRACT TRUNCATED AT 250 WORDS)
Castanheira
I
I
LNETI, Sacavem, Portugal.
Sawas-Dimopoulou
C
C
Paulo
A
A
Neves
M
M
Patricio
L
L
D000137:Acid-Base Imbalance / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001798:Blood Proteins / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D005578:Fosfomycin / Q000737:chemistry; D006868:Hydrolysis; D007668:Kidney / Q000000981:diagnostic imaging* / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D063065:Organophosphonates / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011339:Probenecid / Q000494:pharmacology; D011485:Protein Binding; D011877:Radionuclide Imaging; D051381:Rats; D011933:Reagent Kits, Diagnostic; D014018:Tissue Distribution; D014527:Uric Acid / Q000097:blood
D001798:Blood Proteins; D063065:Organophosphonates; D015609:Organotechnetium Compounds; D011933:Reagent Kits, Diagnostic; C081031:technetium Tc 99m 1,2-dihydroxypropyl-1-phosphonic acid; D014527:Uric Acid; D005578:Fosfomycin; D011339:Probenecid