Radioiodination and astatination of octreotide by conjugation labeling was written by Vaidyanathan, G.;Affleck, D.;Welsh, P.;Srinivasan, A.;Schmidt, M.;Zalutsky, M. R.. And the article was included in Nuclear Medicine and Biology in 2000.Category: iodides-buliding-blocks This article mentions the following:
Octreotide was coupled to 3-iodobenzoyl and 3-iodonicotinoyl moieties to obtain [N-(3-iodobenzoyl)-d-Phe1]octreotide (IBO) and [N-(3-iodonicotinoyl)-d-Phe1]octreotide (INO), resp. The IC50 values for the binding of IBO and INO to CA20948 rat pancreatic tumor membranes were 0.90 and 0.13 nM, resp., compared with 0.35 nM for octreotide itself. Starting from N-succinimidyl 3-[131I]iodobenzoate and N-succinimidyl 5-[131I]iodopyridine-3- carboxylate, [131I]IBO and [131I]INO were prepared in overall radiochem. yields of 35%-50%. Likewise, {N-(3-[211At]astatobenzoyl)-d-Phe1}octreotide ([211At]ABO) was prepared in similar yield from N-succinimidyl 3-[211At]astatobenzoate. In vitro assays with AR42J rat pancreatic tumor cells demonstrated a higher retention of cell-internalized radioiodine activity for [131I]INO compared with [125I]IBO. Tissue distribution studies with both conjugates revealed low levels of activity in the thyroid suggesting that dehalogenation of these peptides was minimal. In the experiment, the researchers used many compounds, for example, 5-Iodonicotinic acid (cas: 15366-65-1Category: iodides-buliding-blocks).
5-Iodonicotinic acid (cas: 15366-65-1) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Category: iodides-buliding-blocks
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com