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[Tc-99m]demotate, a new Tc-99m-based [Tyr(3)]octreotate analogue for the detection of somatostatin receptor-positive tumours: synthesis and preclinical results

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[Tc-99m]demotate, a new Tc-99m-based [Tyr(3)]octreotate analogue for the detection of somatostatin receptor-positive tumours: synthesis and preclinical results (EN)
Nock, B (EN)
Cordopatis, P (EN)
Maina, T (EN)
Nikolopoulou, A (EN)
Chiotellis, E (EN)
Maintas, D (EN)
Sotiriou, P (EN)
Loudos, G (EN)
journalArticle (EN)
2014-03-01T01:52:02Z
2002 (EN)
Demotate is a new tetraamine-functionalised [Tyr(3)]octreotate derivative that binds technetium-99m with a high efficiency under mild conditions. The resulting radioligand, [Tc-99m]Demotate, forms in a high purity and is stable for at least 6 h after labelling. The affinity of the unlabelled peptide for somatostatin receptors is high (IC50=0.13 nM) and comparable to that of [Tyr(3)]octreotate or [Tyr3]octreotide, as demonstrated by competition binding experiments in rat brain cortex or AR42J cell membrane preparations. An equally very high affinity (K-d=0.07 nM) was exhibited by [Tc-99m/Tc-99g]Demotate during saturation binding experiments using rat brain cortex membrane homogenates. The radioligand resisted hydrolytic degradation in mouse plasma and was excreted intact in mouse urine. In vivo, [Tc-99m]Demotate cleared very rapidly from non-target tissues into the bladder via the kidneys, while radioactivity uptake in target organs was very high. In mice bearing the experimental AR42J tumour, [99mTc]Demotate demonstrated a very high tumour uptake at I h p.i. (25%ID/g) that remained high (20%ID/g) at 4 h p.i. This uptake could be effectively blocked by co-injection of a high dose of [Tyr3]octreotate together with the radioligand. High-quality planar and single-photon emission tomographic images were acquired 1 h after injection of [Tc-99m]Demotate in tumour-bearing mice, illustrating the excellent properties of this agent for somatostatin receptor tumour imaging. (EN)
Radiology, Nuclear Medicine & Medical Imaging (EN)
somatostatin receptor (EN)
DIAGNOSIS (EN)
tetraamine chelator (EN)
SCINTIGRAPHY (EN)
tumour imaging (EN)
TUMORS (EN)
Tc-99m (EN)
IN-VITRO (EN)
RADIOPHARMACEUTICALS (EN)
METABOLISM (EN)
AFFINITY (EN)
[Tyr(3)]octreotate (EN)
RADIOTHERAPY (EN)
DERIVATIVES (EN)
BINDING PEPTIDES (EN)
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (EN)
English
SPRINGER-VERLAG (EN)
National Technical University of Athens
Digital Library of National Technical University of Athens | Dspace@NTUA
Κεντρική Βιβλιοθήκη Ε.Μ.Π.
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