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Synthesis, radiochemistry and biological evaluation of a new somatostatin analogue (SDZ 219-387) labelled with technetium-99m.

Abstract
A new derivative of octreotide SDZ 219-387 [PnAO-(D)Phe(1)-octreotide] was synthesized, which binds specifically and with high affinity to somatostatin receptors in vitro (pKi = 9.79 +/- 0.16). This new somatostatin analogue chelates technetium-99m under mild labelling conditions in good yields. The resulting [99mTc]SDZ 219-387 was stable up to 6 h after labelling and could be isolated in a pure radiochemical and chemical form by high-performance liquid chromatographic purification. The intravenous administration of purified [99mTc]SDZ 219-387 revealed that the radioligand was rapidly cleared from circulation, and tumour uptake of 0.38% ID/g was observed at 1.5 h post injection. [99mTc]SDZ 219-387 specifically interacted with somatostatin binding sites on the tumour. However, the radioligand is highly lipophilic and excreted mainly through the hepatobiliary system. As a consequence, [99mTc]SDZ 219-387 exhibits increased background activity and therefore is not appropriate for the in vivo visualization of somatostatin receptor-positive tumours and/or their metastases in the abdomen.
AuthorsT Maina, B Stolz, R Albert, C Bruns, P Koch, H Mäcke
JournalEuropean journal of nuclear medicine (Eur J Nucl Med) Vol. 21 Issue 5 Pg. 437-44 (May 1994) ISSN: 0340-6997 [Print] Germany
PMID8062850 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • (PnAO-(D)Phe(1))octreotide
  • Organotechnetium Compounds
  • Octreotide
Topics
  • Animals
  • Cerebral Cortex (metabolism)
  • Male
  • Models, Chemical
  • Octreotide (analogs & derivatives, chemistry, pharmacokinetics)
  • Organotechnetium Compounds (chemistry, pharmacokinetics)
  • Radioligand Assay
  • Rats
  • Rats, Inbred Lew
  • Rats, Sprague-Dawley

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