Preclinical evaluation of gastrin derivatives labelled with In-111: Radiolabelling, affinity profile and pharmacokinetics in rats

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F14%3A10289751" target="_blank" >RIV/00216208:11160/14:10289751 - isvavai.cz</a>
Result on the web
<a href="http://biomed.papers.upol.cz/pdfs/bio/2014/04/08.pdf" target="_blank" >http://biomed.papers.upol.cz/pdfs/bio/2014/04/08.pdf</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.5507/bp.2013.064" target="_blank" >10.5507/bp.2013.064</a>

Result language
angličtina
Original language name
Preclinical evaluation of gastrin derivatives labelled with In-111: Radiolabelling, affinity profile and pharmacokinetics in rats
Original language description
Background. Cholecystokinin receptor subtype 2 (CCK-2) is overexpressed in various tumours like medullary thyroid carcinomas and small cell lung cancer. Radiolabelled peptides that bind with high affinity and specificity to CCK-2 receptors, thus hold great potential for visualizing such tumours. Methods. We compared four In-111 labelled gastrin analogues, called minigastrins (MG), namely MG11, MG45, MG47 and MG48 linked to metal chelating DOTA in preclinical experiments. The radiolabelled peptides weretested for peptide binding in CCK-2 receptor-bearing cell line AR42J and for their pharmacokinetics in normal rats. Results. The experiments suggest that all gastrin analogues had similar and relatively rapid internalization into AR42J cells. Binding toCCK-2 receptors in AR42J cells was saturable for all agents but there were some differences in receptor affinity. This biodistribution study in rats showed a rapid decrease in blood radioactivity, predominantly renal clearance and saturab
Czech name
—
Czech description
—

Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
—

Project
<a href="/en/project/GAP304%2F10%2F1738" target="_blank" >GAP304/10/1738: Radiolabelled neuropeptides for cancer diagnosis and treatment</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Similar results(10)