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99mTc-DTPA-amino acids conjugate as specific SPECT pharmaceuticals for tumor imaging.

Abstract
(99m)Tc-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 different l-amino acids (methyl tryptophan, and 5-hydroxy tryptophan) and were characterized on the basis of IR, NMR, and Mass spectroscopy. (99m)Tc-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 t(1/2)(F) and t(1/2)(S) were found to be 20 +/- 0.001 min for DTPA-(Me-Trp)(2) and 18 +/- 0.001 min for DTPA-(5HT)(2) and t(1/2) (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 from l-5-hydroxytryptophan exhibited remarkable localization at tumor site; whereas radiotracer derived from l-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 (99m)Tc-DTPA-(Me trp)(2) and 4.97 +/- 0.001 and 5.8 +/- 0.001 at 1 and 4 h after postinjection for (99m)Tc-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.
AuthorsDeepa Sinha, Gauri Shukla, Anjani K Tiwari, Shubhra Chaturvedi, Krishna Chuttani, Harish Chandra, Anil K Mishra
JournalChemical biology & drug design (Chem Biol Drug Des) Vol. 74 Issue 2 Pg. 159-64 (Aug 2009) ISSN: 1747-0285 [Electronic] England
PMID19614681 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Amino Acids
  • Radiopharmaceuticals
  • tryptophan methyl ester
  • Pentetic Acid
  • Tryptophan
  • 5-Hydroxytryptophan
  • Technetium Tc 99m Pentetate
Topics
  • 5-Hydroxytryptophan (analogs & derivatives, chemistry, pharmacokinetics)
  • Amino Acids (chemistry)
  • Animals
  • Carcinoma, Ehrlich Tumor (diagnostic imaging)
  • Cell Line, Tumor
  • Humans
  • Mice
  • Mice, Inbred BALB C
  • Pentetic Acid (analogs & derivatives, chemistry, pharmacokinetics)
  • Rabbits
  • Radiopharmaceuticals (chemistry, pharmacokinetics)
  • Technetium Tc 99m Pentetate (chemistry)
  • Tissue Distribution
  • Tomography, Emission-Computed, Single-Photon
  • Tryptophan (analogs & derivatives, chemistry, pharmacokinetics)

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