Receptor Affinity and Preclinical Biodistribution of Radiolabeled Somatostatin Analogs

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F12%3A10124213" target="_blank" >RIV/00216208:11160/12:10124213 - isvavai.cz</a>

Výsledek na webu

<a href="http://ar.iiarjournals.org/content/32/3/761.full" target="_blank" >http://ar.iiarjournals.org/content/32/3/761.full</a>

DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Receptor Affinity and Preclinical Biodistribution of Radiolabeled Somatostatin Analogs

Popis výsledku v původním jazyce

In this study, we investigated the relationship between affinity to somatostatin receptor subtype2 (SSTR2) and uptake of radioactivity from a group of radiolabeled somatostatin analogues in somatostatin receptor-rich tissues of rats. Organs with a high density of somatostin receptors (namely the adrenals and pancreas bearing mainly SSTR2; this receptor subtype is also the most abundant in somatostatin receptor-positive tumors) were chosen as markers of specific binding of the peptides in vivo. Accumulations of radioactivity in these organs 24 h and 48 h after intravenous administration of six In-111-labeled octreotide and octreotate derivatives with predominant affinity to SSTR2 were correlated with affinity to SSTR2, determined in vitro (IC50 values).For correlation between adrenal uptake of radioactivity and IC50, the best fit for exponential dependence was found; for that of pancreas, however, linear dependence was the most suitable. In cases where the values for the peptide with a

Název v anglickém jazyce

Receptor Affinity and Preclinical Biodistribution of Radiolabeled Somatostatin Analogs

Popis výsledku anglicky

In this study, we investigated the relationship between affinity to somatostatin receptor subtype2 (SSTR2) and uptake of radioactivity from a group of radiolabeled somatostatin analogues in somatostatin receptor-rich tissues of rats. Organs with a high density of somatostin receptors (namely the adrenals and pancreas bearing mainly SSTR2; this receptor subtype is also the most abundant in somatostatin receptor-positive tumors) were chosen as markers of specific binding of the peptides in vivo. Accumulations of radioactivity in these organs 24 h and 48 h after intravenous administration of six In-111-labeled octreotide and octreotate derivatives with predominant affinity to SSTR2 were correlated with affinity to SSTR2, determined in vitro (IC50 values).For correlation between adrenal uptake of radioactivity and IC50, the best fit for exponential dependence was found; for that of pancreas, however, linear dependence was the most suitable. In cases where the values for the peptide with a

Druh

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

CEP obor

FD - Onkologie a hematologie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2012

Kód důvěrnosti údajů

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

Název periodika

Anticancer Research

ISSN

0250-7005

e-ISSN

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Svazek periodika

32

Číslo periodika v rámci svazku

3

Stát vydavatele periodika

GR - Řecká republika

Počet stran výsledku

6

Strana od-do

761-766

Kód UT WoS článku

000301619200007

EID výsledku v databázi Scopus

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