18F-labeled sufentanil for PET-imaging of μ-opioid receptors

被引：10
作者：
Henriksen, G
Platzer, S
Hauser, A
Willoch, F
Berthele, A
Schwaiger, M
Wester, HE
机构：
[1] Tech Univ Munich, Klinikum Rechts Isar, Dept Nucl Med, D-81675 Munich, Germany
[2] Tech Univ Munich, Klinikum Rechts Isar, Dept Neurol, D-81675 Munich, Germany
[3] Natl Hosp Norway, Dept Nucl Med, N-0027 Oslo, Norway
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 07期
关键词：
opioid receptor imaging; positron emission tomography; 4-anilidopiperidines; sufentanil; fluorine-18;
D O I：
10.1016/j.bmcl.2005.02.049
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of an F-18-labeled sufentanil analogue with apparent high mu-opioid receptor selectivity is reported. Intravenous injection of N-[4-(methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenyl-2-(+/-)-[F-18]fluoropropan-amide in mice resulted in high brain uptake and a regional brain activity distribution corresponding to the mu-opioid receptor expression pattern. The developed ligand is a promising tracer for extended protocols in mu-opioid receptor mapping and quantitation with positron emission tomography. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1773 / 1777
页数：5
相关论文
共 19 条
[1]   Mu-opioid receptor binding measured by [11C]carfentanil positron emission tomography is related to craving and mood in alcohol dependence [J].
Bencherif, B ;
Wand, GS ;
McCaul, ME ;
Kim, YK ;
Iigin, N ;
Dannals, RF ;
Frost, JJ .
BIOLOGICAL PSYCHIATRY, 2004, 55 (03) :255-262
[2]   Pain activation of human supraspinal opioid pathways as demonstrated by [11C]-carfentanil and positron emission tomography (PET) [J].
Bencherif, B ;
Fuchs, PN ;
Sheth, R ;
Dannals, RF ;
Campbell, JN ;
Frost, JJ .
PAIN, 2002, 99 (03) :589-598
[3]   ENANTIOMERS OF DIASTEREOMERIC CIS-N-[1-(2-HYDROXY-2-PHENYLETHYL)-3-METHYL-4-PIPERIDYL]-N-PHENYLPROPANAMIDES - SYNTHESIS, X-RAY-ANALYSIS, AND BIOLOGICAL-ACTIVITIES [J].
BRINE, GA ;
STARK, PA ;
LIU, Y ;
CARROLL, FI ;
SINGH, P ;
XU, H ;
ROTHMAN, RB .
JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (09) :1547-1557
[4]   QUANTITATION OF MU-OPIOID RECEPTOR (MOR-1) MESSENGER-RNA IN SELECTED REGIONS OF THE RAT CNS [J].
BRODSKY, M ;
ELLIOTT, K ;
HYNANSKY, A ;
JENAB, S ;
INTURRISI, CE .
NEUROREPORT, 1995, 6 (05) :725-729
[5]  
COMETTAMORINI C, 1992, MOL PHARMACOL, V41, P185
[6]  
DANNALS RF, 1985, INT J APPL RADIAT IS, V36, P303, DOI 10.1016/0020-708X(85)90089-4
[7]   THE INSITU GENERATION AND TRAPPING OF SOME FLUORINE-SUBSTITUTED KETENES [J].
DOLBIER, WR ;
LEE, SK ;
PHANSTIEL, O .
TETRAHEDRON, 1991, 47 (12-13) :2065-2072
[8]   MU-OPIATE RECEPTORS MEASURED BY POSITRON EMISSION TOMOGRAPHY ARE INCREASED IN TEMPORAL-LOBE EPILEPSY [J].
FROST, JJ ;
MAYBERG, HS ;
FISHER, RS ;
DOUGLASS, KH ;
DANNALS, RF ;
LINKS, JM ;
WILSON, AA ;
RAVERT, HT ;
ROSENBAUM, AE ;
SNYDER, SH ;
WAGNER, HN .
ANNALS OF NEUROLOGY, 1988, 23 (03) :231-237
[9]   Effects of buprenorphine maintenance dose on μ-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteers [J].
Greenwald, MK ;
Johanson, CE ;
Moody, DE ;
Woods, JH ;
Kilbourn, MR ;
Koeppe, RA ;
Schuster, CR ;
Zubieta, JK .
NEUROPSYCHOPHARMACOLOGY, 2003, 28 (11) :2000-2009
[10]  
Henriksen G, 2004, EUR J NUCL MED MOL I, V31, pS250
12