Fluoro-norchloroepibatidine: preclinical assessment of acute toxicity.

abstract：OBJECTIVES:To compare the radiolabeling performance, stability, and practical efficacy of the chelators CHX-A″-DTPA and H4octapa with the therapeutic radiometal (90)Y. METHODS:The bifunctional chelators p-SCN-Bn-H4octapa and p-SCN-Bn-CHX-A″-DTPA were conjugated to the HER2-targeting antibody trastuzumab. The resulting...

journal_title：Nuclear medicine and biology

authors： Price EW,Edwards KJ,Carnazza KE,Carlin SD,Zeglis BM,Adam MJ,Orvig C,Lewis JS

更新日期：2016-09-01 00:00:00

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

authors： Iznaga Escobar N,Morales A,Núñez G

更新日期：1996-07-01 00:00:00

abstract：INTRODUCTION:Altered lipid metabolism and subsequent changes in cellular lipid composition have been observed in prostate cancer cells, are associated with poor clinical outcome, and are promising targets for metabolic therapies. This study reports for the first time on the synthesis of a phospholipid radiotracer based...

journal_title：Nuclear medicine and biology

authors： Kwan KH,Burvenich IJG,Centenera MM,Goh YW,Rigopoulos A,Dehairs J,Swinnen JV,Raj GV,Hoy AJ,Butler LM,Scott AM,White JM,Ackermann U

更新日期：2020-11-28 00:00:00

abstract：:In connection with pretargeting, an amine-derivatized morpholino phosphorodiamidate oligomer (NH(2)-cMORF) was conjugated conventionally with p-isothiocyanate benzyl-DTPA (p-SCN-Bn-DTPA). However, after (111)In radiolabeling, unexpected label instability was observed. To understand this instability, the NH(2)-cMORF an...

journal_title：Nuclear medicine and biology

authors： Liu G,Dou S,Liu Y,Liang M,Chen L,Cheng D,Greiner D,Rusckowski M,Hnatowich DJ

更新日期：2011-02-01 00:00:00

abstract：:Brofaromine (4-5(-methoxy-7-bromobenzofuranyl)-2-piperidine-HCl) is a potent and selective inhibitor of monoamine oxidase (MAO) A. Two methods for its synthesis and a preliminary positron emission tomography (PET) evaluation in monkey brain are described. The first method, at low carrier concentration of CO2, consiste...

journal_title：Nuclear medicine and biology

authors： Ametamey SM,Beer HF,Guenther I,Antonini A,Leenders KL,Waldmeier PC,Schubiger PA

更新日期：1996-04-01 00:00:00

abstract：UNLABELLED:The radiolabelled bombesin analogue AMBA shows high potential for diagnosis and treatment of prostate and breast cancer, but the influence of different chelators, which differ in terms of radiochemical reactivity and stability, have not been explored so far. In order to find the best suitable chelator for la...

journal_title：Nuclear medicine and biology

authors： Asti M,Iori M,Capponi PC,Atti G,Rubagotti S,Martin R,Brennauer A,Müller M,Bergmann R,Erba PA,Versari A

更新日期：2014-01-01 00:00:00

abstract：:Ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinoline-3-carboxylic acid), a widely-prescribed antibiotic, was labeled with fluorine-18 with the aim to perform positron emission tomography studies in humans for pharmacokinetic measurements. Due to a lack of chemical activation of ciproflox...

journal_title：Nuclear medicine and biology

authors： Langer O,Mitterhauser M,Brunner M,Zeitlinger M,Wadsak W,Mayer BX,Kletter K,Müller M

更新日期：2003-04-01 00:00:00

abstract：:Positron-emission tomography (PET) provides potential in neuropsychiatric drug development by expanding knowledge of drug action in the living human brain and reducing time consumption and costs. The 5-hydroxytryptamine(1A) (5-HT(1A)) receptor is of central interest as a target for the treatment of anxiety, depression...

journal_title：Nuclear medicine and biology

authors： Andrée B,Halldin C,Thorberg SO,Sandell J,Farde L

更新日期：2000-07-01 00:00:00

abstract：OBJECTIVES:Positron emission tomography (PET) using O-(2-[(18)F]fluoroethyl)-l-tyrosine (FET) has been successfully employed in the diagnostic workup of brain tumors. Knowledge on the mechanisms of the uptake of radiolabeled amino acids into thyroidal tissues and well-differentiated thyroid carcinomas is limited. We th...

journal_title：Nuclear medicine and biology

authors： Prante O,Bläser D,Maschauer S,Kuwert T

更新日期：2007-04-01 00:00:00

abstract：:This paper describes the radiosynthesis of [(11)C]CGP62349, a potential ligand to assess GABA(B) receptors in vivo. (11)C was introduced by O-methylation of the corresponding des-methyl precursor, namely CGP67780. The final product was obtained with a reliable method in good yield. The radioligand was tested in monkey...

journal_title：Nuclear medicine and biology

authors： Todde S,Moresco RM,Fröstl W,Stampf P,Matarrese M,Carpinelli A,Magni F,Galli Kienle M,Fazio F

更新日期：2000-08-01 00:00:00

abstract：:The in vitro metabolism of 1-(4-[(18)F]fluoromethylbenzyl)-4-phenylpiperazine ([(18)F]1) and 1-(4-[(18)F]fluorobenzyl)-4-phenylpiperazine ([(18)F]2) was investigated using mouse liver S9 fraction. Results were compared to those of in vivo metabolism using mouse blood and bone and to in vitro metabolism using mouse liv...

journal_title：Nuclear medicine and biology

authors： Ryu EK,Choe YS,Kim DH,Ko BH,Choi Y,Lee KH,Kim BT

更新日期：2006-02-01 00:00:00

abstract：:Sixteen patients with colorectal cancer were administered 37-74 MBq (1 mg) of radioiodinated B72.3 monoclonal antibody. Pharmacokinetic analysis was carried out on plasma and urine samples. Elimination from the plasma was biexponential with a mean T1/2 alpha of 3.7 h and T1/2 beta of 62.4 h. The plasma clearance was f...

journal_title：Nuclear medicine and biology

authors： Reilly RM,Kirsh J,Gallinger S,Thiessen JJ,Damani M,Hay K,Polihronis J,Schmocker B,Odze R,Houle S

更新日期：1993-01-01 00:00:00

abstract：:A new 99mTc labelling method using a cleavable chelator, RP-1, was developed. In this study Balb/c mice with ovarian carcinoma xenografts received various Fab' fragments labelled with 99mTc either directly or via RP-1. Kidney uptake was significantly lower for the RP-1 linked conjugates. Tumour uptake showed no signif...

journal_title：Nuclear medicine and biology

authors： Tibben JG,Massuger LF,Boerman OC,Claessens RA,Borm GF,Pak KY,Koenders EB,Corstens FH

更新日期：1994-01-01 00:00:00

abstract：INTRODUCTION:Rodent models are extensively used to assess the biochemical and physiological changes associated with aging. They play a major role in the development of therapies for age-related pathologies such as Parkinson's disease. To validate the usefulness of these animal models in aging or age-related disease res...

journal_title：Nuclear medicine and biology

authors： Niñerola-Baizán A,Rojas S,Roé-Vellvé N,Lomeña F,Ros D,Pavía J

更新日期：2015-04-01 00:00:00

abstract：:We compared the influence of three different catechol-O-methyltransferase (COMT) inhibitors (CGP 28014, OR-611 and Ro 40-7592) on the metabolism of no-carrier-added (NCA) 6-[18F]fluoro-L-dopa (6-FDOPA) in one Rhesus monkey. All three COMT inhibitors improved 6-FDOPA availability in plasma, increased the specific uptak...

journal_title：Nuclear medicine and biology

authors： Günther I,Psylla M,Reddy GN,Antonini A,Vontobel P,Reist HW,Zollinger A,Nickles RJ,Beer HF,Schubiger PA

更新日期：1995-10-01 00:00:00

abstract：:Technetium-99m-modified polylysine (MPL) is a mild and efficient method for cell labeling that is easily applicable to human lymphocytes. 99mTc-MPL uptake is maximal in 40 min at room temperature. Cell labeling efficiency (from 60 to 80%) increases with rising concentrations of cells and labeling agent. In vitro stabi...

journal_title：Nuclear medicine and biology

authors： Delmon-Moingeon LI,Mahmood A,Davison A,Jones AG

更新日期：1996-01-01 00:00:00

abstract：INTRODUCTION:⁶⁸Ga-labeled RGD peptides in combination with PET allow non-invasive determination of α(v)β₃ integrin expression which is highly increased during tumor-induced angiogenesis. The aim of this study was to synthesize and evaluate two RGD peptides containing alternative chelating systems, namely [⁶⁸Ga]NS₃-RGD-...

journal_title：Nuclear medicine and biology

authors： Knetsch PA,Petrik M,Rangger C,Seidel G,Pietzsch HJ,Virgolini I,Decristoforo C,Haubner R

更新日期：2013-01-01 00:00:00

abstract：:The imaging of the distribution of beta-amyloid (Abeta) plaques in the brain is becoming an important diagnostic modality in Alzheimer's disease (AD). Here, we synthesized novel benzothiophene derivatives and labeled them with (18)F for the potential diagnostic imaging of AD patients using positron emission tomography...

journal_title：Nuclear medicine and biology

authors： Chang YS,Jeong JM,Lee YS,Kim HW,Ganesha RB,Kim YJ,Lee DS,Chung JK,Lee MC

更新日期：2006-08-01 00:00:00

abstract：UNLABELLED:In recent years, several PET and SPECT studies have shown loss of striatal dopamine transporter (DAT) binding in amphetamine (AMPH) users. However, the use of DAT SPECT tracers to detect AMPH-induced changes in DAT binding has not been validated. We therefore examined if repeated administration of D-AMPH or ...

journal_title：Nuclear medicine and biology

authors： Booij J,de Bruin K,Gunning WB

更新日期：2006-04-01 00:00:00

abstract：:In vivo pharmacokinetic and brain binding characteristics of [18F]RP 62203, a selective high-affinity serotonergic 5-HT2A receptor antagonist, were assessed in the rat following intravenous injection of trace amount of the radioligand. The radioactive distribution profile observed in the brain 60 min after injection w...

journal_title：Nuclear medicine and biology

authors： Besret L,Dauphin F,Huard C,Lasne MC,Vivet R,Mickala P,Barbelivien A,Baron JC

更新日期：1996-02-01 00:00:00

abstract：:Targeted Auger Therapy represents great potential for the therapy of diseases which require a high degree of selectivity on the cellular level (e.g. for therapy of metastatic cancers). Due to their high Linear Energy Transfer (LET), Auger emitters, combined with selective biological systems which enable delivery of ra...

journal_title：Nuclear medicine and biology

authors： Filosofov D,Kurakina E,Radchenko V

更新日期：2020-12-13 00:00:00

abstract：:At present, P-glycoprotein (P-gp) function can be studied using positron emission tomography (PET) together with a labelled P-gp substrate such as R-[11C]verapamil. Such a tracer is, however, less suitable for investigating P-gp (over)expression. Laniquidar is a third-generation P-gp inhibitor, which has been used in ...

journal_title：Nuclear medicine and biology

authors： Luurtsema G,Schuit RC,Klok RP,Verbeek J,Leysen JE,Lammertsma AA,Windhorst AD

更新日期：2009-08-01 00:00:00

abstract：BACKGROUND:Cu-diacetyl-bis(N4-methylthiosemicarbazone) [Cu-ATSM], although excellent for oncology applications, may not be suitable for delineating cardiovascular or neurological hypoxia. For this reason, new Cu hypoxia positron emission tomography (PET) imaging agents are being examined to search for a higher selectiv...

journal_title：Nuclear medicine and biology

authors： McQuade P,Martin KE,Castle TC,Went MJ,Blower PJ,Welch MJ,Lewis JS

更新日期：2005-02-01 00:00:00

abstract：:[(123)I]AIBZM, (S)-5-[(123)I]-Iodo-N-[(1-ethyl-2-pyrrolidinyl)]methyl-4-amine-2-methoxybenzamide is a derivative with high affinity for the D2 receptor. Labeling was achieved by the Iodogen method. The in vivo affinity for the D2 receptor and the biological characteristics were performed in rats. The brain uptake of [...

journal_title：Nuclear medicine and biology

authors： Li H,Gildehaus FJ,Dresel S,Patt JT,Shen M,Zhu T,Liu B,Tang Z,Tatsch K,Hahn K

更新日期：2001-05-01 00:00:00

abstract：:Copper-64-labeled monoclonal antibodies (mAbs) have previously demonstrated unexpectedly effective tumor control in rodent models of cancer at relatively low tumor-absorbed radiation doses. This property has been associated with delivery platforms resulting in cellular internalization. The purpose of the present studi...

journal_title：Nuclear medicine and biology

authors： Bryan JN,Jia F,Mohsin H,Sivaguru G,Miller WH,Anderson CJ,Henry CJ,Lewis MR

更新日期：2005-11-01 00:00:00

abstract：:Liver accumulation of 99mTc-DL-homocysteine (99mTc-Hcy), which had been found to accumulate in several experimental tumors, was studied using experimental hepatitis models of rats. The distribution of this compound in liver of rats treated with CCl4 (25-100 microL/100 g body weight) was more than five times higher tha...

journal_title：Nuclear medicine and biology

authors： Takeda A,Okumura H,Okada S

更新日期：1993-11-01 00:00:00

abstract：: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...

journal_title：Nuclear medicine and biology

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

更新日期：2002-05-01 00:00:00

abstract：INTRODUCTION:Image-derived input functions (IDIFs) represent a promising non-invasive alternative to arterial blood sampling for quantification in positron emission tomography (PET) studies. However, routine applications in patients and longitudinal designs are largely missing despite widespread attempts in healthy sub...

journal_title：Nuclear medicine and biology

authors： Hahn A,Nics L,Baldinger P,Wadsak W,Savli M,Kraus C,Birkfellner W,Ungersboeck J,Haeusler D,Mitterhauser M,Karanikas G,Kasper S,Frey R,Lanzenberger R

更新日期：2013-04-01 00:00:00

abstract：:Structural variations of the nicotinic acetylcholine receptor radioligand N-[(11)C]methyl-epibatidine were made to form (11)C-labeled N-methyl-norchloroepibatidine (N-methyl-NorchloroEPB) and N-methyl-2-(2-pyridyl)-7-azabicyclo[2.2.1]heptane (N-methyl-2PABH). Radiosyntheses were performed by methylation with high radi...

journal_title：Nuclear medicine and biology

authors： Spang JE,Patt JT,Westera G,Schubiger PA

更新日期：2000-04-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the biodistribution and localization of an anti-inflammatory nonapeptide coupled to synovial targeting peptide (HAP-1) in rat adjuvant-induced arthritis. PROCEDURE:N(ε)-functionalized histidine derivative was coupled to the N-terminus of core peptide (CP) and HAP-1 to a...

journal_title：Nuclear medicine and biology

authors： Ali M,Vanniasinghe A,Kumar V,Barnett R,Alberto R,Manolios N

更新日期：2011-07-01 00:00:00