Synthesis of p-aminohippuric acid analog and its labeling by technetium-99m.
A procedure is described for the synthesis of p-[(bisacarboxymethyl)aminomethyl carbamino] hippuric acid (PAHIDA). The compound was identified by i.r. and NMR spectroscopy. A lyophilized complex was prepared and labeled with 99mTc. The purity of the preparation is better than 98%. The stability of the 99mTc-PAHIDA complex is achieved 8 h after labeling. Biodistribution tested on white rats shows a maximum accumulation in kidneys of 6-10% within 2 min after injection, while the accumulation in the liver is 2-4% of the administrated dose. Preliminary clinical studies of 99mTc-PAHIDA on patients and its comparison with 131I-hippuran showed that the 99Tc-PAHIDA preparation has excellent characteristics for visualization of kidneys. However, it has slightly slower urinary elimination compared to hippuran, which it makes possible to use PAHIDA as a replacement of hippuran to a certain extent.
Zmbova
B
B
Institute for Radioisotopes, Boris Kidric Institute of Nuclear Sciences, Vinca, Belgrade, Yugoslavia.
Djokić
D
D
Bogdanova
V
V
Tadzer
I
I
Ajdinović
B
B
Rastovac
M
M
D000328:Adult; D000618:Aminohippuric Acids / Q000138:chemical synthesis*; D000818:Animals; D005260:Female; D006801:Humans; D007465:Iodohippuric Acid; D007668:Kidney / Q000000981:diagnostic imaging; D008297:Male; D009393:Nephritis / Q000000981:diagnostic imaging; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D015609:Organotechnetium Compounds; D011877:Radionuclide Imaging; D051381:Rats; D013667:Technetium; D014018:Tissue Distribution; D010130:p-Aminohippuric Acid / Q000138:chemical synthesis* / Q000493:pharmacokinetics
D000618:Aminohippuric Acids; D009942:Organometallic Compounds; D015609:Organotechnetium Compounds; C059603:technetium Tc 99m 4-((bis(carboxymethyl)aminomethyl)carbamino)hippuric acid; D007465:Iodohippuric Acid; D013667:Technetium; D010130:p-Aminohippuric Acid