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- Title
<sup>99m</sup>Tc-DTPA-Amino Acids Conjugate as Specific SPECT Pharmaceuticals for Tumor Imaging.
- Authors
Sinha, Deepa; Shukla, Gauri; Tiwari, Anjani K.; Chaturvedi, Shubhra; Chuttani, Krishna; Chandra, Harish; Mishra, Anil K.
- Abstract
99mTc-Diethylene triamine pentaacetic acid-bis (amide) conjugates have been synthesized and evaluated as a potential radiopharmaceutical for tumor imaging. The compounds were synthesized by the condensation reaction of DTPA bis(anhydride) with differentl-amino acids (methyl tryptophan, and 5-hydroxy tryptophan) and were characterized on the basis of IR, NMR, and Mass spectroscopy. 99mTc-labeled compounds were found stable for about 24 h under physiological conditions with more than 95% radiolabeling yield. Blood kinetic studies of all these complexes showed a bi-exponential pattern as well as quick wash out from the blood circulation. The biological t1/2(F) and t1/2(S) were found to be 20 ± 0.001 min for DTPA-(Me-Trp)2 and 18 ± 0.001 min for DTPA-(5HT)2 and t1/2 (slow) 5 h 45 min ± 0.001, 5 h 30 ± 0.001 min for DTPA-(Me-Trp)2, and DTPA-(5HT)2, respectively. Imaging and biodistribution studies were performed in mice bearing Ehrlich ascites tumor (EAT) tumors in right thigh. Radioconjugate derived froml-5-hydroxytryptophan exhibited remarkable localization at tumor site; whereas radiotracer derived froml-methyl tryptophan shows relatively less accumulation at the tumor site. Tumor-to-muscles ratios were 5.07 ± 0.001, and 4.2 ± 0.001 at 1 and 4 h for 99mTc-DTPA-(Me trp)2 and 4.97 ± 0.001 and 5.8 ± 0.001 at 1 and 4 h after postinjection for 99mTc-DTPA-(5HT)2, respectively. The preliminary results with these amino acid based ligands are encouraging to carrying out further in vivo experiments for targeted tumor imaging.
- Subjects
AMIDES; AMINO acids; RADIOPHARMACEUTICALS; MASS spectrometry; NUCLEAR magnetic resonance; HYDROXYTRYPTOPHAN
- Publication
Chemical Biology & Drug Design, 2009, Vol 74, Issue 2, p159
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/j.1747-0285.2009.00839.x