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Radioiodination and astatination of octreotide by conjugation labeling.

Publication ,  Journal Article
Vaidyanathan, G; Affleck, D; Welsh, P; Srinivasan, A; Schmidt, M; Zalutsky, MR
Published in: Nucl Med Biol
May 2000

Octreotide was coupled to 3-iodobenzoyl and 3-iodonicotinoyl moieties to obtain [N-(3-iodobenzoyl)-D-Phe(1)]octreotide (IBO) and [N-(3-iodonicotinoyl)-D-Phe(1)]octreotide (INO), respectively. The IC(50) values for the binding of IBO and INO to CA20948 rat pancreatic tumor membranes were 0.90 and 0.13 nM, respectively, compared with 0.35 nM for octreotide itself. Starting from N-succinimidyl 3-[(131)I]iodobenzoate and N-succinimidyl 5-[(131)I]iodopyridine-3- carboxylate, [(131)I]IBO and [(131)I]INO were prepared in overall radiochemical yields of 35%-50%. Likewise, ¿N-(3-[(211)At]astatobenzoyl)-D-Phe(1)¿octreotide ([(211)At]ABO) was prepared in similar yield from N-succinimidyl 3-[(211)At]astatobenzoate. In vitro assays with AR42J rat pancreatic tumor cells demonstrated a higher retention of cell-internalized radioiodine activity for [(131)I]INO compared with [(125)I]IBO. Tissue distribution studies with both conjugates revealed low levels of activity in the thyroid suggesting that dehalogenation of these peptides was minimal.

Duke Scholars

Published In

Nucl Med Biol

DOI

ISSN

0969-8051

Publication Date

May 2000

Volume

27

Issue

4

Start / End Page

329 / 337

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Rats
  • Octreotide
  • Nuclear Medicine & Medical Imaging
  • Mice
  • Isotope Labeling
  • Iodine Radioisotopes
  • Astatine
  • Animals
 

Citation

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Vaidyanathan, G., Affleck, D., Welsh, P., Srinivasan, A., Schmidt, M., & Zalutsky, M. R. (2000). Radioiodination and astatination of octreotide by conjugation labeling. Nucl Med Biol, 27(4), 329–337. https://doi.org/10.1016/s0969-8051(00)00098-6
Vaidyanathan, G., D. Affleck, P. Welsh, A. Srinivasan, M. Schmidt, and M. R. Zalutsky. “Radioiodination and astatination of octreotide by conjugation labeling.Nucl Med Biol 27, no. 4 (May 2000): 329–37. https://doi.org/10.1016/s0969-8051(00)00098-6.
Vaidyanathan G, Affleck D, Welsh P, Srinivasan A, Schmidt M, Zalutsky MR. Radioiodination and astatination of octreotide by conjugation labeling. Nucl Med Biol. 2000 May;27(4):329–37.
Vaidyanathan, G., et al. “Radioiodination and astatination of octreotide by conjugation labeling.Nucl Med Biol, vol. 27, no. 4, May 2000, pp. 329–37. Pubmed, doi:10.1016/s0969-8051(00)00098-6.
Vaidyanathan G, Affleck D, Welsh P, Srinivasan A, Schmidt M, Zalutsky MR. Radioiodination and astatination of octreotide by conjugation labeling. Nucl Med Biol. 2000 May;27(4):329–337.
Journal cover image

Published In

Nucl Med Biol

DOI

ISSN

0969-8051

Publication Date

May 2000

Volume

27

Issue

4

Start / End Page

329 / 337

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Rats
  • Octreotide
  • Nuclear Medicine & Medical Imaging
  • Mice
  • Isotope Labeling
  • Iodine Radioisotopes
  • Astatine
  • Animals