Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1831283 | Nuclear Instruments and Methods in Physics Research Section A: Accelerators, Spectrometers, Detectors and Associated Equipment | 2007 | 5 Pages |
Abstract
S-EOE-MAG3-β-alanine-CCK4 vector (S-EOE-MAG3-β-alanine: S-(1-ethoxyethyl) mercaptoacetyltriglycyl -β-alanine and CCK4: Trp-Met-Asp-Phe-NH2) was obtained by successive condensations of activated amino acids on resin with high chemical purity. This biovector was complexed at high dilution scale with 99mTc as well as at ponderable level with 185/187Re and 99Tc. In particular, this biovector was efficiently labelled with 99mTc (yield>95%) in one step under pH 7-8 and 45 °C conditions and then injected, In vivo, for biodistribution and targeting of pancreatic adenocarcinoma tumoral grafts (AR4-J). 99mTc-MAG3-β-alanine-CCK4 exhibits remarkable biological properties related to its low background noise resulting from the fast blood clearance (tissular distribution half-life â10 min, elimination half-life â 20 min), low hepatic uptake (0.03% injected dose/g of tissue 2 h after injection) and good affinity for the CCKB receptors (IC50=8Ã10â8 M) expressed by tumoral cells.
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Authors
Hafid Belhadj-Tahar, Jean-Paul Esquerre, Yvon Coulais,