Abstract：
:By variation of reaction parameters iodination of 3-(9,10-didehydro-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea (lisuride) was performed with the radiohalogen [123I]iodine (t1/2 = 13.3 h). For comparative experiments and stability studies the beta(-)-emitting radioisotope [131I]iodine (t1/2 = 8.04 d) was also used. Reaction occurs at the activated position 2 of the molecule, thus leading to [123I]3-(9,10-didehydro-2-iodo-6-methyl-8 alpha-ergolinyl)-1,1-diethylurea ([123I]2-iodo-lisuride, [123I]ILIS) or the analogous [131I]iodine-labeled compound, respectively. Electrophilic radioactive species were generated by oxidation of no-carrier-added (n.c.a.) iodide with IODOGEN (1,3,4,6-tetrachloro-3 alpha,6 alpha-diphenylglycouril) fixed on the glass wall of the reaction vial prior to iodination. After optimization of reaction parameters [123I]2-iodo-lisuride after HPLC-purification was obtained with radiochemical yields of 70 +/- 5% and a radiochemical purity of > 97%. In n.c.a. syntheses, specific activities of the product were in the range between 4440 and 7400 GBq/mumol (120-200 Ci/mumol) corresponding to 50-85% of the theoretical value.
journal_name
Nucl Med Bioljournal_title
Nuclear medicine and biologyauthors
Bier D,Dutschka K,Knust EJdoi
10.1016/0969-8051(96)00018-2subject
Has Abstractpub_date
1996-04-01 00:00:00pages
373-6issue
3eissn
0969-8051issn
1872-9614pii
0969-8051(96)00018-2journal_volume
23pub_type
杂志文章abstract：:The imaging of apoptosis represents an attractive diagnostic goal in the area of tumor therapy, degenerative diseases and organ transplantation. Since caspases play a key role during the early period of the intracellular signal cascade of cells undergoing apoptosis we considered benzyloxycarbonyl-Val-Ala-DL-Asp(O-meth...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(01)00247-5
更新日期：2001-10-01 00:00:00
abstract：:The syntheses and radiolabelling of 27 new N-(alkylaminoalkyl)-4-methoxy-, -4-hydroxy-, and -4-aminobenzamides are described and evaluated in C57B1/6 mice with subcutaneously transplanted B16 melanoma in order to screen the optimal chemical structure for melanoma scintigraphy. Using T1(TFA)3 for 131I- labelling, a ser...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(97)00024-3
更新日期：1997-07-01 00:00:00
abstract：:We prepared 5-HT(1A) receptor ligands (S)-N-[[1-(2-phenylethyl)pyrrolidin-2-yl]methyl]-3-[11C]methylthiobenzamide ([11C](S)-PPMMB) (Ki = 4.3 nM) and the less active [(11)C](R)-PPMMB (Ki = 160 nM) by reduction of the disulfide dimer and subsequent [(11)C]methylation of demethyl (S)- and (R)-PPMMB, respectively. Both ra...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(02)00305-0
更新日期：2002-08-01 00:00:00
abstract：:Three new radiolabeled compounds, [(11)C]SNC80 ((+)-4-[(αR)-α-{(2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl}-3-[(11)C]methoxybenzyl-N,N-diethylbenzamide), N,N-diethyl-4-[3-methoxyphenyl-1-[(11)C]methylpiperidin-4-ylidenemethyl)benzamide and N,N-diethyl-4-[(1-[(11)C]methylpiperidin-4-ylidene)phenylmethyl]benzamide, were ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2010.06.002
更新日期：2010-11-01 00:00:00
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
doi：10.1016/s0969-8051(97)00160-1
更新日期：1998-04-01 00:00:00
abstract：:The anabolism of isotopically labeled amino acids was compared between the cerebrum and the cerebellum in conscious rat at three feeding conditions. After L-[2-18F]fluorophenylalanine and L-[2,6-3H]phenylalanine injections, the incorporation rate of both radioactivity into protein fraction showed no difference between...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)90085-x
更新日期：1994-10-01 00:00:00
abstract：:A computer controlled [15O]H2O injection system has been designed for multiple bolus injections during PET cerebral blood flow studies. The system is housed in a lead safe, and radiation exposure to nearby personnel is low; we have measured rates of approx. 100 microSv/h (10 mR/h) during 2 min of [15O]H2O production a...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)00085-x
更新日期：1995-02-01 00:00:00
abstract：INTRODUCTION:Hypoxia plays a negative role in the clinical management of cancer. Detection of hypoxic status of a cancer is important for selecting patients for hypoxia directed therapy. Though [(18)F]fluoromisonidazole ([(18)F]FMISO), a PET radiopharmaceutical, is presently being used in the clinic for the detection o...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2014.04.103
更新日期：2014-08-01 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
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2012.09.006
更新日期：2013-01-01 00:00:00
abstract：INTRODUCTION:The purpose of the study was to examine potential of 131I-labeled chitosan hydrogels (Chi) for treatment of liver cancer. METHODS:Orthotopic hepatoma was induced by McA-RH7777-fLuc cells (1×107) that were injected into the left hepatic lobe of rats. Ten days later, tumor-bearing rats evidenced by biolumin...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2017.05.006
更新日期：2017-09-01 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
pub_type： 杂志文章
doi：10.1016/s0969-8051(00)00121-9
更新日期：2000-07-01 00:00:00
abstract：:To improve standardization in analytical reagents we investigated Chloramine-T radioiodination (125I) of several biomolecules based on the use of a single amount of the oxidizing agent Chloramine-T as the limiting reagent being exhausted during the course of the reaction. Whenever the labeling yield resulted in less t...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(01)00261-x
更新日期：2001-11-01 00:00:00
abstract：INTRODUCTION:The neurohistological findings in patients treated with targeted beta emitters such as (131)I are poorly described. We report a histopathologic analysis from patients treated with combined external beam therapy and a brachytherapy consisting of a (131)I-labeled monoclonal antibody (mAb) injected into surgi...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2007.01.009
更新日期：2007-05-01 00:00:00
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
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2016.06.004
更新日期：2016-09-01 00:00:00
abstract：INTRODUCTION:We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ("GABA shift") using [18F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [18F]FMZ binding were compared to that of [18F]FM...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2016.11.003
更新日期：2017-02-01 00:00:00
abstract：:To fully exploit the potential of positron emission tomography (PET) imaging to assess drug distribution and pharmacokinetics in the central nervous system, the contribution of radiometabolites to the PET signal has to be determined for correct interpretation of data. However, radiosynthesis and extensive study of rad...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2020.08.001
更新日期：2020-01-01 00:00:00
abstract：:Pretargeted tumour imaging was performed in nude mice bearing subcutaneous LS174T human colon cancer xenografts with streptavidin-CC49 monoclonal antibody and 111In-DTPA-biocytin. Mice were administered 250 micrograms of streptavidin-CC49, followed 6 or 9 days later by 40 ng (250 microCi) of 111In-DTPA-biocytin. Tumor...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(96)00022-4
更新日期：1996-05-01 00:00:00
abstract：:The pharmacokinetics and internal radionuclide therapy of intraperitoneally administrated (188)Re-N,N-bis(2-mercaptoethyl)-N',N'-diethylethylenediamine (BMEDA)-labeled pegylated liposomal doxorubicin ((188)Re-DXR-liposome) were investigated in the C26 murine colon carcinoma ascites mouse model. After intraperitoneal a...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2008.09.005
更新日期：2008-11-01 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
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.12.002
更新日期：2006-02-01 00:00:00
abstract：:We have synthesized three different PET ligands to investigate the physiological function of metabotropic glutamate subtype 5 receptors (mGluR5) in vivo: 2-[(11)C]methyl-6-(2-phenylethynyl)pyridine ([(11)C]MPEP), 2-(2-(3-[(11)C]methoxyphenyl)ethynyl)pyridine ([(11)C]M-MPEP) and 2-(2-(5-[(11)C]methoxypyridin-3-yl)ethyn...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2005.05.004
更新日期：2005-08-01 00:00:00
abstract：:Rhenium-186 (Re-186) hydroxyethylidene diphosphonate (HEDP) has been shown to localize in metastatic foci within bone in a manner similar to Tc-99m bone-seeking agents. Usually, in the preparation of diagnostic Tc-99m radiopharmaceuticals, the concentration of Tc is at trace level (10(-8) M). However, large amounts of...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(99)00007-4
更新日期：1999-05-01 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
pub_type： 杂志文章
doi：10.1016/s0969-8051(00)00080-9
更新日期：2000-04-01 00:00:00
abstract：INTRODUCTION:Radiolabeled 2-nitroimidazoles (azomycins) are a prominent class of biomarkers for PET imaging of hypoxia. [18F]Fluoro-azomycin-α-arabinoside ([18F]FAZA) - already in clinical use - may be seen as α-configuration nucleoside, but enters cells only via diffusion and is not transported by cellular nucleoside ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2016.08.005
更新日期：2016-12-01 00:00:00
abstract：:The specific binding of [(11)C]doxepin, which has been used as a radioligand for mapping histamine H(1) receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [(11)C]doxepin uptake was reduced by treatment with cold doxepin and two H(1) receptor antagonists, but not...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2003.11.005
更新日期：2004-05-01 00:00:00
abstract：INTRODUCTION:Derived from heavy chain only camelid antibodies, ~15-kDa single-domain antibody fragments (sdAbs) are an attractive platform for developing molecularly specific imaging probes and targeted radiotherapeutics. The rapid tumor accumulation and normal tissue clearance of sdAbs might be ideal for use with 211A...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2017.09.003
更新日期：2018-01-01 00:00:00
abstract：:The synthetic porphyrins, N-benzyl-5,10,15,20-tetrakis (4-carboxyphenyl) porphine (N-bzHTCPP) and N-4-nitrobenzyl-5-(4-carboxyphenyl)-10,15,20-tris(4-sulfophenyl) porphine (N-bzHCS3P), represent excellent radiocopper chelating agents that may find utility in antibody-mediated diagnosis and/or therapy. N-bzHCS3P was co...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(96)00215-6
更新日期：1997-02-01 00:00:00
abstract：:18Fluoro-norchloroepibatidine (exo-2-(6-fluoro-3-pyridyl)-7-azabicyclo-[2.2.1]heptane [NFEP]), a labeled derivative of epibatidine, has shown promise for imaging brain nicotinic acetylcholine receptors with PET. We determined the dose-dependent effects of NFEP in conscious rats. NFEP (1.5 microg/kg; administered intra...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(97)00120-0
更新日期：1997-11-01 00:00:00
abstract：INTRODUCTION:Prognostic markers for progression of polycystic kidney disease (PKD) are limited. We evaluated the potential of early para-[(18)F]fluorohippurate ([(18)F]PFH) positron emission tomography (PET) renography to predict future progression of PKD in Han:SPRD rats with slowly progressive autosomal dominant PKD....
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/j.nucmedbio.2015.10.002
更新日期：2016-01-01 00:00:00
abstract：:A new tetrahydrazido-germanium (GeTH) ligand was synthesized, characterized and complexed with 99mTc. The negatively charged 99mTc-chelate was shown to form in high yields at neutral pH in the absence of other reducing agents and exhibits high in vitro and in vivo stability. ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/0969-8051(94)90184-8
更新日期：1994-11-01 00:00:00
abstract：:The present study was undertaken to investigate if pretreatment with pharmacological agents could change the organ uptake of 11C-labelled L-DOPA, and especially if the urinary excretion could be decreased. L-[beta-11C]DOPA was injected IV into unanesthetized Sprague-Dawley rats. After 20 min the rats were decapitated ...
journal_title：Nuclear medicine and biology
pub_type： 杂志文章
doi：10.1016/s0969-8051(96)00149-7
更新日期：1997-01-01 00:00:00
