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

Kód výsledku v IS VaVaI

RIV/00216208:11160/14:10289751 - isvavai.cz

Výsledek na webu

http://biomed.papers.upol.cz/pdfs/bio/2014/04/08.pdf

DOI - Digital Object Identifier

10.5507/bp.2013.064

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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

Název v anglickém jazyce

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

Popis výsledku anglicky

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

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

GAP304/10/1738: Radioaktivně značené neuropeptidy cílené pro diagnostiku a terapii nádorů

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Biomedical Papers

ISSN

1213-8118

e-ISSN

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Svazek periodika

158

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

CZ - Česká republika

Počet stran výsledku

8

Strana od-do

544-551

Kód UT WoS článku

000347173200008

EID výsledku v databázi Scopus

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