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[99mTc]Demotate, a new 99mTc-based [Tyr3]octreotate analogue for the detection of somatostatin receptor-positive tumours: Synthesis and preclinical results

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dc.contributor.author Maina, T en
dc.contributor.author Nock, B en
dc.contributor.author Nikolopoulou, A en
dc.contributor.author Sotiriou, P en
dc.contributor.author Loudos, G en
dc.contributor.author Maintas, D en
dc.contributor.author Cordopatis, P en
dc.contributor.author Chiotellis, E en
dc.date.accessioned 2014-03-01T01:17:20Z
dc.date.available 2014-03-01T01:17:20Z
dc.date.issued 2002 en
dc.identifier.issn 03406997 en
dc.identifier.uri https://dspace.lib.ntua.gr/xmlui/handle/123456789/14463
dc.subject 99mTc en
dc.subject [Tyr3]octreotate en
dc.subject Somatostatin receptor en
dc.subject Tetraamine chelator en
dc.subject Tumour imaging en
dc.subject.other demotate tc 99m en
dc.subject.other octreotate[3 tyrosine] en
dc.subject.other octreotide[3 tyrosine] en
dc.subject.other somatostatin receptor en
dc.subject.other technetium 99m en
dc.subject.other tyrosine derivative en
dc.subject.other unclassified drug en
dc.subject.other 3 Tyr octreotide en
dc.subject.other 3-Tyr-octreotide en
dc.subject.other cyclopeptide en
dc.subject.other diagnostic agent en
dc.subject.other drug derivative en
dc.subject.other octreotate, Tyr(3) en
dc.subject.other octreotate, Tyr(3)- en
dc.subject.other octreotide en
dc.subject.other octreotide, iodoTyr(3) en
dc.subject.other octreotide, iodoTyr(3)- en
dc.subject.other somatostatin receptor 2 en
dc.subject.other technetium complex en
dc.subject.other technetium Tc 99m demotate en
dc.subject.other amine en
dc.subject.other demotate en
dc.subject.other animal cell en
dc.subject.other animal model en
dc.subject.other animal tissue en
dc.subject.other article en
dc.subject.other brain cortex en
dc.subject.other brain homogenate en
dc.subject.other cell membrane en
dc.subject.other controlled study en
dc.subject.other drug clearance en
dc.subject.other drug degradation en
dc.subject.other drug distribution en
dc.subject.other drug stability en
dc.subject.other drug synthesis en
dc.subject.other drug uptake en
dc.subject.other female en
dc.subject.other high performance liquid chromatography en
dc.subject.other IC 50 en
dc.subject.other in vivo study en
dc.subject.other internalization en
dc.subject.other isotope labeling en
dc.subject.other male en
dc.subject.other mouse en
dc.subject.other nonhuman en
dc.subject.other radioactivity en
dc.subject.other rat en
dc.subject.other receptor affinity en
dc.subject.other single photon emission computer tomography en
dc.subject.other animal en
dc.subject.other cell culture en
dc.subject.other chemical model en
dc.subject.other in vitro study en
dc.subject.other metabolic clearance rate en
dc.subject.other metabolism en
dc.subject.other methodology en
dc.subject.other nude mouse en
dc.subject.other pancreas tumor en
dc.subject.other protein binding en
dc.subject.other reproducibility en
dc.subject.other scintiscanning en
dc.subject.other sensitivity and specificity en
dc.subject.other synthesis en
dc.subject.other tissue distribution en
dc.subject.other Wistar rat en
dc.subject.other animal experiment en
dc.subject.other imaging en
dc.subject.other tumor en
dc.subject.other Animals en
dc.subject.other Cerebral Cortex en
dc.subject.other Female en
dc.subject.other Isotope Labeling en
dc.subject.other Male en
dc.subject.other Metabolic Clearance Rate en
dc.subject.other Mice en
dc.subject.other Mice, Nude en
dc.subject.other Models, Chemical en
dc.subject.other Octreotide en
dc.subject.other Organotechnetium Compounds en
dc.subject.other Pancreatic Neoplasms en
dc.subject.other Peptides, Cyclic en
dc.subject.other Protein Binding en
dc.subject.other Rats en
dc.subject.other Rats, Wistar en
dc.subject.other Receptors, Somatostatin en
dc.subject.other Reproducibility of Results en
dc.subject.other Sensitivity and Specificity en
dc.subject.other Tissue Distribution en
dc.subject.other Tumor Cells, Cultured en
dc.title [99mTc]Demotate, a new 99mTc-based [Tyr3]octreotate analogue for the detection of somatostatin receptor-positive tumours: Synthesis and preclinical results en
heal.type journalArticle en
heal.identifier.primary 10.1007/s00259-002-0782-9 en
heal.identifier.secondary http://dx.doi.org/10.1007/s00259-002-0782-9 en
heal.publicationDate 2002 en
heal.abstract Demotate is a new tetraamine-functionalised [Tyr3]octreotate derivative that binds technetium-99m with a high efficiency under mild conditions. The resulting radioligand, [99mTc]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 [Tyr3]octreotate or [Tyr3]octreotide, as demonstrated by competition binding experiments in rat brain cortex or AR42J cell membrane preparations. An equally very high affinity (Kd=0.07 nM) was exhibited by [99mTc/99gTc]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, [99mTc]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 1 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 [99mTc]Demotate in tumour-bearing mice, illustrating the excellent properties of this agent for somatostatin receptor tumour imaging. en
heal.journalName European Journal of Nuclear Medicine en
dc.identifier.doi 10.1007/s00259-002-0782-9 en
dc.identifier.volume 29 en
dc.identifier.issue 6 en
dc.identifier.spage 742 en
dc.identifier.epage 753 en


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