N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) potential delta-opioid receptor PET ligands.


:The properties of two prospective positron emission tomography (PET) ligands for the delta-opioid receptor, N1'-fluoroethyl-naltrindole (BU97001) and N1'-fluoroethyl-(14-formylamino)-naltrindole (BU97018) were investigated. Both were antagonists in the mouse vas deferens, and showed high affinity and selectivity, 1.81 nM and 3.09 nM respectively. [3H]BU97001 binding to rat whole brain was also of high affinity, K(D) of 0.42 nM of and B(MAX) of 59.95 fmol mg of protein(-1). In autoradiographic studies, it was found to bind to brain areas previously shown to be associated with the delta-opioid receptor and good correlations were found to exist with naltrindole and DPDPE. BU97018 and especially BU97001 appear to show good potential as delta-opioid receptor PET ligands with the incorporation of 18F.


Nucl Med Biol


Tyacke RJ,Robinson ES,Schnabel R,Lewis JW,Husbands SM,Nutt DJ,Hudson AL





Has Abstract


2002-05-01 00:00:00














  • Preliminary assessment of extrastriatal dopamine D-2 receptor binding in the rodent and nonhuman primate brains using the high affinity radioligand, 18F-fallypride.

    abstract::We have identified the value of 18F-fallypride [(S)-N-[(1-allyl-2-pyrrolidinyl)methyl]-5-(3-[18F]fluoropropyl)-2, 3-dimethoxybenzamide], as a dopamine D-2 receptor radiotracer for the study of striatal and extrastriatal receptors. Fallypride exhibits high affinities for D-2 and D-3 subtypes and low affinity for D-4 (3...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Mukherjee J,Yang ZY,Brown T,Lew R,Wernick M,Ouyang X,Yasillo N,Chen CT,Mintzer R,Cooper M

    更新日期:1999-07-01 00:00:00

  • Cardiac lymphatic dynamics after ischemia and reperfusion--experimental model.

    abstract::ABSTRACT. The aim of the present study was to investigate the lymphatic cardiac circulation in an experimental model of ischemia plus reperfusion in mongrel dogs (Canis familiaris L). As radiotracer we used 0.2-0.25 ml (111 MBq) of 99mTc-Re2S7 colloid (+/-10 microm), injected subcapsullary below the second diagonal of...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Santos AC,de Lima JJ,Botelho MF,Pacheco MF,Sousa P,Bernardo J,Ferreira N,Gonçalves L,Aguiar J,Providência LA,Pauwels EK

    更新日期:1998-10-01 00:00:00

  • Synthesis of [18F]RGD-K5 by catalyzed [3 + 2] cycloaddition for imaging integrin αvβ3 expression in vivo.

    abstract::In the last few years click chemistry reactions, and in particular copper-catalyzed cycloadditions have been used extensively for the preparation of new bioconjugated molecules such as (18)F-radiolabeled radiopharmaceuticals for positron emission tomography (PET). This study is focused on the synthesis of the Siemens ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Mirfeizi L,Walsh J,Kolb H,Campbell-Verduyn L,Dierckx RA,Feringa BL,Elsinga PH,de Groot T,Sannen I,Bormans G,Celen S

    更新日期:2013-07-01 00:00:00

  • In vivo characterization of radioiodinated (+)-2-[4-(4-iodophenyl) piperidino] cyclohexanol as a potential sigma-1 receptor imaging agent.

    abstract::In this study, the (+)-enantiomer of radioiodinated 2-[4-(4-iodophenyl)piperidino]cyclohexanol [(+)-[(125)I]-p-iodovesamicol] [(+)-[(125)I]pIV], which is reported to bind with high affinity to sigma-1 receptors in vitro, was tested for its usefulness in imaging sigma-1 receptors in the central nervous system (CNS) in ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Akhter N,Shiba K,Ogawa K,Kinuya S,Nakajima K,Mori H

    更新日期:2007-08-01 00:00:00

  • 65Zn uptake by liver of rats fed 3'-methyl-dimethylaminoazobenzene.

    abstract::The uptake of 65Zn, determined by gamma-counting and also by autoradiography, significantly increased with the increasing level of metallothionein in liver 4 weeks after the start of feeding a diet containing 3'-methyl-dimethylaminoazobenzene (3'-Me-DAB), at which time the serum gamma-glutamyl transpeptidase activity ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Takeda A,Tamano H,Ohnuma M,Okada S

    更新日期:1995-04-01 00:00:00

  • In vivo binding of [11C]nemonapride to sigma receptors in the cortex and cerebellum.

    abstract::Radiolabeled nemonapride (NEM, YM-09151-2) is widely used as a representative dopamine D2-like receptor ligand in pharmacological and neurological studies, and 11C-labeled analog ([11C]NEM) has been developed for positron emission tomography (PET) studies. The aim of this study was to evaluate whether [11C]NEM binds i...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Ishiwata K,Senda M

    更新日期:1999-08-01 00:00:00

  • A fast chemoenzymatic synthesis of [11C]-N5,N10-methylenetetrahydrofolate as a potential PET tracer for proliferating cells.

    abstract:INTRODUCTION:Thymidylate synthase and folate receptors are well-developed targets of cancer therapy. Discovery of a simple and fast method for the conversion of 11CH3Ito[11C]-formaldehyde (11CH2O) encouraged us to label the co-factor of this enzyme. Preliminary studies conducted on cell lines have demonstrated a prefer...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Saeed M,Tewson TJ,Erdahl CE,Kohen A

    更新日期:2012-07-01 00:00:00

  • [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), whi...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


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

    更新日期:2008-07-01 00:00:00

  • Impact of benzodiazepines on brain FDG-PET quantification after single-dose and chronic administration in rats.

    abstract:INTRODUCTION:Current guidelines for brain PET imaging advice against the injection of diazepam prior to brain FDG-PET examination in order to avoid possible interactions of benzodiazepines with the radiotracer uptake. Nevertheless, many patients undergoing PET studies are likely to be under chronic treatment with benzo...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Silva-Rodríguez J,García-Varela L,López-Arias E,Domínguez-Prado I,Cortés J,Pardo-Montero J,Fernández-Ferreiro A,Ruibal Á,Sobrino T,Aguiar P

    更新日期:2016-12-01 00:00:00

  • Radiosynthesis and biological evaluation of alpha-[F-18]fluoromethyl phenylalanine for brain tumor imaging.

    abstract:OBJECTIVES:Radiolabeled amino acids have proven utility for imaging brain tumors in humans, particularly those that target system L amino acid transport. We have prepared the novel phenylalanine analogue, (FMePhe, 9), as part of an effort to develop new system L tracers that can be prepared in high radiochemical yield ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Huang C,Yuan L,Rich KM,McConathy J

    更新日期:2013-05-01 00:00:00

  • Synthesis and in vivo evaluation of [O-methyl-11C](2R,4R)-4-hydroxy-2-[2-[2-[2-(3-methoxy)phenyl]ethyl]phenoxy]ethyl-1-methylpyrrolidine as a 5-HT2A receptor PET ligand.

    abstract::The serotonin2A (5-HT2A) receptor is implicated in the pathophysiology of schizophrenia and mood disorders, and in vivo studies of this receptor would be of value in studying the pathophysiology of these disorders and in measuring the relationship of clinical response to receptor occupancy for 5-HT2A antagonists such ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Kumar JS,Prabhakaran J,Erlandsson K,Majo VJ,Simpson NR,Pratap M,Van Heertum RL,Mann JJ,Parsey RV

    更新日期:2006-05-01 00:00:00

  • Cellular penetration and nuclear importation properties of 111In-labeled and 123I-labeled HIV-1 tat peptide immunoconjugates in BT-474 human breast cancer cells.

    abstract:INTRODUCTION:Our objective was to compare the cell penetration and nuclear importation properties of 111In-labeled and 123I-labeled immunoconjugates (ICs) composed of 16-mer peptides (GRKKRRQRRRPPQGYG) derived from HIV-1 transactivator of transcription (tat) protein and anti-mouse IgG (mIgG) in BT-474 breast cancer (BC...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Cornelissen B,Hu M,McLarty K,Costantini D,Reilly RM

    更新日期:2007-01-01 00:00:00

  • Micromethod for quantification of SH groups generated after reduction of monoclonal antibodies.

    abstract::A simple, rapid, and reproducible micromethod for quantification of sulfhydryl (SH) groups generated after reduction of monoclonal antibody (MAb) disulfide bonds with 2-mercaptoethanol (2-ME) is described. The number of SH groups per molecule of antibody in the 2-ME and in the other reducing agents was calculated from...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Iznaga Escobar N,Morales A,Núñez G

    更新日期:1996-07-01 00:00:00

  • (E)-[125I]-5-AOIBV: a SPECT radioligand for the vesicular acetylcholine transporter.

    abstract::The premise that, over the course of Alzheimer's disease (AD), changes in the levels of the vesicular acetylcholine transporter (VAChT) occur in parallel with changes to other cholinergic marker proteins provides the basis for the applicability of benzovesamicol derivatives as radioligands for AD studies by single pho...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Emond P,Mavel S,Zea-Ponce Y,Kassiou M,Garreau L,Bodard S,Drossard ML,Chalon S,Guilloteau D

    更新日期:2007-11-01 00:00:00

  • Synthesis and preliminary evaluation of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)guanine ([18F]FHBG): a new potential imaging agent for viral infection and gene therapy using PET.

    abstract::Synthesis and preliminary biological evaluation of 9-(4-[18F]-fluoro-3-hydroxymethylbutyl)-guanine ([18F]FHBG) is reported. 9-(4-Hydroxy-3-hydroxymethylbutyl)-guanine (penciclovir) 4 was converted to 9-[N2, O-bis-(methoxytrityl)-3-(tosylmethybutyl)]guanine 7 by treatment with methoxytrityl chloride followed by tosylat...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Alauddin MM,Conti PS

    更新日期:1998-04-01 00:00:00

  • A bolus/infusion paradigm for the novel NMDA receptor SPET tracer [123I]CNS 1261.

    abstract::We have previously performed quantitative kinetic modeling of [(123)I]CNS 1261, a new SPET ligand for the MK801 intrachannel site of the NMDA receptor. We now report a bolus-infusion protocol, which eliminates the need for arterial blood sampling. Dynamic SPET scanning and venous blood sampling were performed in 7 hea...

    journal_title:Nuclear medicine and biology

    pub_type: 临床试验,杂志文章


    authors: Bressan RA,Erlandsson K,Mulligan RS,Gunn RN,Cunningham VJ,Owens J,Cullum ID,Ell PJ,Pilowsky LS

    更新日期:2004-02-01 00:00:00

  • System a amino acid transport-targeted brain and systemic tumor PET imaging agents 2-amino-3-[(18)F]fluoro-2-methylpropanoic acid and 3-[(18)F]fluoro-2-methyl-2-(methylamino)propanoic acid.

    abstract:INTRODUCTION:Amino acid based radiotracers target tumor cells through increased uptake by membrane-associated amino acid transport (AAT) systems. In the present study, four structurally related non-natural (18)F-labeled amino acids, (R)- and (S)-[(18)F]FAMP 1 and (R)- and (S)-[(18)F]MeFAMP 2 have been prepared and eval...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Yu W,McConathy J,Olson JJ,Goodman MM

    更新日期:2015-01-01 00:00:00

  • Sequence-specific binding and cleavage of duplex DNA by a radioiodinated, intercalator-linked, triplex-forming oligonucleotide.

    abstract::Applications of oligodeoxynucleotides to modulate gene expression have been the subject of much recent research. We have sought to develop a method to permanently inactivate a gene, or potentially kill cells containing abnormal genes. In this report, we show that a DNA intercalator conjugated to a triplex-forming olig...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Orson FM,McShan WM,Kinsey BM

    更新日期:1996-05-01 00:00:00

  • [125/123I] 5-Iodo-3-pyridyl ethers. syntheses and binding to neuronal nicotinic acetylcholine receptors.

    abstract::Three 3-pyridyl ether nicotinic ligands-(S)-5-Iodo-3-[(2-pyrrolidinyl)-methoxy]pyridine (5-iodo-A-85865), (S)-5-Iodo-3-[1-(methyl)-2-pyrrolidinyl-methoxy]pyridine (5-Iodo-A-84543), and (S)-5-iodo-3-[1-methyl-(2-azetidinyl)-methoxy]pyridine (5-iodo-N-Me-A-85380) were labeled with I-125/I-123, and their ability to label...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Fan H,Scheffel UA,Rauseo P,Xiao Y,Dogan AS,Yokoi F,Hilton J,Kellar KJ,Wong DF,Musachio JL

    更新日期:2001-11-01 00:00:00

  • Synthesis and preliminary evaluation of para- and meta-[18F]fluorobenzylguanidine.

    abstract::meta-[18F]Fluorobenzylguanidine ([18F]MFBG) and para-[18F]fluorobenzylguanidine ([18F]PFBG) were synthesized in three steps beginning with a fluoro for nitro exchange reaction on 3- and 4-nitrobenzonitrile, respectively. Overall radiochemical yields were 10-15% for [18F]MFBG and 50-55% for [18F]PFBG in a total synthes...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Garg PK,Garg S,Zalutsky MR

    更新日期:1994-01-01 00:00:00

  • Imaging recognition of multidrug resistance in human breast tumors using 99mTc-labeled monocationic agents and a high-resolution stationary SPECT system.

    abstract::Imaging recognition of multidrug-resistance by 99mTc-labeled sestamibi, tetrofosmin and furifosmin in mice bearing human breast tumors was evaluated using a high-resolution SPECT, FASTSPECT. Imaging results showed that the washout rates in drug-resistant MCF7/D40 tumors were significantly greater than that in drug-sen...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Liu Z,Stevenson GD,Barrett HH,Kastis GA,Bettan M,Furenlid LR,Wilson DW,Woolfenden JM

    更新日期:2004-01-01 00:00:00

  • Effect of arteriovenous difference in measuring renal function by single-injection plasma clearance: role of bolus.

    abstract::Error estimates for arteriovenous difference were calculated by two models, a lag time model and a compartmental model, using Tc99m-diethylenetriaminepentaacetic acid (DTPA) plasma clearance curves from 40 subjects and Tc99m-MAG3 (mercaptoacetyltriglycine) curves from 18 subjects. It was found that correcting for the ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Russell CD,Dubovsky EV

    更新日期:1999-08-01 00:00:00

  • Biodistribution of (125)I-labeled anti-endoglin antibody using SPECT/CT imaging: Impact of in vivo deiodination on tumor accumulation in mice.

    abstract:INTRODUCTION:Radiolabeled antibodies directed against endoglin (CD105) are promising tools for imaging and antiangiogenic cancer therapy. To validate iodinated antibodies as reliable tracers, we investigated the influence of the radiolabeling method (direct or indirect) on their in vivo stability. METHODS:Anti-CD105 m...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Karmani L,Levêque P,Bouzin C,Bol A,Dieu M,Walrand S,Vander Borght T,Feron O,Grégoire V,Bonifazi D,Michiels C,Lucas S,Gallez B

    更新日期:2016-07-01 00:00:00

  • A comparison of four PET tracers for brain hypoxia mapping in a rodent model of stroke.

    abstract:INTRODUCTION:Severe brain hypoxia in the territory of the occluded artery is a key feature of ischemic stroke. This region can be imaged using positron emission tomography (PET) and the standard hypoxia radiotracer (18)F-fluoromisonidazole ((18)F-FMISO). However, the utility of (18)F-FMISO is limited by its slow accumu...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Williamson DJ,Ejaz S,Sitnikov S,Fryer TD,Sawiak SJ,Burke P,Baron JC,Aigbirhio FI

    更新日期:2013-04-01 00:00:00

  • Biological studies of radiolabeled glucose analogues iodinated in positions 3, 4 or 6.

    abstract::The aim of this study was to assess the biological behavior of new radiolabeled glucose analogues proposed as tracers of glucose uptake in vivo and iodinated in position 3, 4, or 6. Biological results obtained in vitro on adipocytes and erythrocytes and in vivo in mice were compared to those obtained with the gold-sta...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Perret P,Ghezzi C,Ogier L,Abbadi M,Morin C,Mathieu JP,Fagret D

    更新日期:2004-02-01 00:00:00

  • Determination of specific radioactivity for (76)Br-labeled compounds measuring the ratio between (76)Br and (79)Br using packed capillary liquid chromatography mass spectrometry.

    abstract::Packed capillary liquid chromatography with electrospray mass spectrometry was used for direct determination of the specific radioactivity by calculation of isotope ratios between the (76)Br- and (79)Br-labeled analogues of N-((3-aminomethyl)benzyl)-4-bromobenzamide. Using 20 microL injections on packed capillary colu...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Forngren BH,Yngve U,Forngren T,Långström B

    更新日期:2000-11-01 00:00:00

  • An alumina ceramic target vessel for the remote production of metallic radionuclides by in situ target dissolution.

    abstract:INTRODUCTION:As the use of metallic radionuclides increases, so does the demand for a simple production method. In this study, we demonstrated an in situ target processing concept for automated metallic radionuclide production without the use of any robotic device. METHODS:An alumina ceramic vessel for a vertical irra...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Nagatsu K,Suzuki H,Fukada M,Minegishi K,Tsuji A,Fukumura T

    更新日期:2012-11-01 00:00:00

  • A new nucleophilic fluorine-18 labeling method for aliphatic mesylates: reaction in ionic liquids shows tolerance for water.

    abstract::[see text for equation] Nucleophilic [(18)F]fluorination of some halo- and mesyloxyalkanes to the corresponding [(18)F]fluoroalkanes with fluoride-18 obtained from an (18)O(p,n) [(18)F]F reaction, using an ionic liquid as a reaction medium, has been studied as a new method for fluorine-18 labeling. Of the various ioni...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Kim DW,Choe YS,Chi DY

    更新日期:2003-05-01 00:00:00

  • Comparison of the distribution of radioiodinated di- and tri-hydroxyphenylethylene estrogens in the immature female rat.

    abstract::The uptake, retention and tissue to blood ratios of two non-steroidal, 125I-labeled iodoestrogens, an iodotrihydroxyphenylethylene, 2-iodo-1,2-bis(4-hydroxyphenyl)-2-(3-hydroxyphenyl)ethylene and an iododihydroxyphenylethylene, 2-iodo-1,1-bis(4-hydroxyphenyl)-2-phenylethylene, were compared after intraperitoneal injec...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Desombre ER,Pribish J,Hughes A

    更新日期:1995-07-01 00:00:00

  • Intraarticular and intravenous administration of 99MTc-HMPAO-labeled human mesenchymal stem cells (99MTC-AH-MSCS): In vivo imaging and biodistribution.

    abstract:INTRODUCTION:Therapeutic application of intravenous administered (IV) human bone marrow-derived mesenchymal stem cells (ahMSCs) appears to have as main drawback the massive retention of cells in the lung parenchyma, questioning the suitability of this via of administration. Intraarticular administration (IAR) could be ...

    journal_title:Nuclear medicine and biology

    pub_type: 杂志文章


    authors: Meseguer-Olmo L,Montellano AJ,Martínez T,Martínez CM,Revilla-Nuin B,Roldán M,Mora CF,López-Lucas MD,Fuente T

    更新日期:2017-03-01 00:00:00