当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > [11C]-MeJDTic: a novel radioligand for kappa-opioid receptor positron emission tomography imaging.

[11C]-MeJDTic: a novel radioligand for kappa-opioid receptor positron emission tomography imaging.

Abstract：

INTRODUCTION:Radiopharmaceuticals that can bind selectively the kappa-opioid receptor may present opportunities for staging clinical brain disorders and evaluating the efficiency of new therapies related to stroke, neurodegenerative diseases or opiate addiction. The N-methylated derivative of JDTic (named MeJDTic), which has been recently described as a potent and selective antagonist of kappa-opioid receptor in vitro, was labeled with carbon-11 and evaluated for in vivo imaging the kappa-opioid receptor in mice. METHODS:[(11)C]-MeJDTic was prepared by methylation of JDTic with [(11)C]-methyl triflate. The binding of [(11)C]-MeJDTic to kappa-opioid receptor was investigated ex vivo by biodistribution and competition studies using nonfasted male CD1 mice. RESULTS:[(11)C]-MeJDTic exhibited a high and rapid distribution in peripheral organs. The uptake was maximal in lung where the kappa receptor is largely expressed. [(11)C]-MeJDTic rapidly crossed the blood-brain barrier and accumulated in the brain regions of interest (hypothalamus). The parent ligand remained the major radioactive compound in brain during the experiment. Chase studies with U50,488 (a kappa referring agonist), morphine (a mu agonist) and naltrindole (a delta antagonist) demonstrated that this uptake was the result of specific binding to the kappa-opioid receptor. CONCLUSION:These findings suggested that [(11)C]-MeJDTic appeared to be a promising selective "lead" radioligand for kappa-opioid receptor PET imaging.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Poisnel G,Oueslati F,Dhilly M,Delamare J,Perrio C,Debruyne D,Barré L

doi

10.1016/j.nucmedbio.2008.02.010

subject

Has Abstract

pub_date

2008-07-01 00:00:00

pages

561-9

issue

5

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(08)00062-0

journal_volume

35

pub_type

杂志文章

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