- Development of a resonant-type microwave reactor and its application to the synthesis of positron emission tomography radiopharmaceuticals
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Microwave technology has been successfully applied to enhance the effectiveness of radiolabeling reactions. The use of a microwave as a source of heat energy can allow chemical reactions to proceed over much shorter reaction times and in higher yields tha
- Kimura, Hiroyuki,Yagi, Yusuke,Ohneda, Noriyuki,Odajima, Hiro,Ono, Masahiro,Saji, Hideo
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- Solid-phase synthesis and fluorine-18 radiolabeling of cycloRGDyK
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Solid-phase peptide synthesis, head-to-tail cyclization, and subsequent radiolabeling provided a reproducible, simple, rapid synthetic method to generate the cyclic peptide radiotracer cRGDyK([18F]FBA). Herein is reported the first on-resin cyclization and 18F-radiolabeling of a cyclic peptide (cRGDyK) in an overall peptide synthesis yield of 88% (cRGDyK(NH2)) and subsequent radiolabeling yield of 14 ± 2% (decay corrected, n = 4). This approach is generally applicable to the development of an automated process for the synthesis of cyclic radiolabeled peptides for positron emission tomography (PET).
- Davis, Ryan A.,Lau, Kevin,Hausner, Sven H.,Sutcliffe, Julie L.
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- A simplified protocol for the automated production of succinimidyl 4-[ 18F]fluorobenzoate on an IBA Synthera module
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The important peptide labelling reagent succinimidyl 4-[ 18F]fluorobenzoate ([18F]SFB) has been synthesised in 75-85% decay corrected radiochemical yield using the IBA Synthera platform (IBA Cyclotron Solutions, Louvain-la-neuve, Bel
- Ackermann, Uwe,Yeoh, Shinn Dee,Sachinidis, John I.,Poniger, Stan S.,Scott, Andrew M.,Tochon-Danguy, Henri J.
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- Synthesis of 18F labelled FK960, a candidate anti-dementia drug, and PET studies in conscious monkeys
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The present study demonstrated the synthesis and in vivo study of 18F-labeled N-(4-acetyl-1-piperazinyl)-p-fluorobenzamide (FK960) which is a novel anti-dementia drug candidate. [18F]FK960 was prepared by a one-pot, three reaction sequence, using nucleophilic fluorination, with an automated synthetic apparatus using either ethyl-4-trimethylammonium triflate (1a) or ethyl-4-nitrobenzoate (lb) as the precursor for labeling. Though la gave a higher yield, the specific activity was 50-100 fold higher with 1b. The radiochemical yield of [18F]FK960 was 7-15% (EOB) and the specific activity ranged from 2.0-60.2GBq/μmol depending on the amount of F-18 used. The synthesis time was 2.2-2.9 h. The obtained [18F]FK960 was injected into 3 conscious monkeys (100-120MBq/kg body weight), and distribution images and pharmacokinetic data for [18F]FK960 showed similar uptake in different brain regions and 3-fold higher levels of [18F]FK960 in blood relative to brain. Copyright
- Murakami, Yoshihiro,Nishimura, Shintaro,Noda, Akihiro,Harada, Norihiro,Tsukada, Hideo
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- Preparation and evaluation of fluorine-18-labeled insulin as a molecular imaging probe for studying insulin receptor expression in tumors
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A convenient emulsion-based labeling method was used to synthesize fluorine-18-labeled insulin specifically B1-(4-[18F] fluorobenzoyl)insulin (18F-4b) in 6% overall radiochemical yield in 240 min. In vitro screening in MCF
- Kim, Dong Hyun,Blacker, Megan,Valliant, John F.
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- In vivo positron emission tomography (PET) imaging with an αvβ6 specific peptide radiolabeled using 18F-"click" chemistry: Evaluation and comparison with the corresponding 4-[18F]fluorobenzoyl- and 2-[18
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Numerous radiolabeled peptides have been utilized for in vivo imaging of a variety of cell surface receptors. For applications in PET using [ 18F]fluorine, peptides are radiolabeled via a prosthetic group approach. We previously developed solut
- Hausner, Sven H.,Marik, Jan,Gagnon, M. Karen J.,Sutcliffe, Julie L.
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- Synthesis and in vitro evaluation of 18F- and 19F-labeled insulin: A new radiotracer for PET-based molecular imaging studies
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A new and regioselective strategy was developed for the preparation of fluorine-18-labeled insulin as a novel positron emission tomography (PET) tracer. [18F]-4-Fluorobenzoic acid (4-18FBA), which was produced in 83 ± 8% yield (n = 1
- Guenther, Katharina J.,Yoganathan, Sabesan,Garofalo, Robert,Kawabata, Thomas,Strack, Thomas,Labiris, Renée,Dolovich, Myrna,Chirakal, Raman,Valliant, John F.
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- Preparation of the novel fluorine-18-labeled VIP analog for PET imaging studies using two different synthesis methods
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Vasoactive intestinal peptide (VIP) receptors are expressed on various tumor cells in much higher density than somatostatin receptors, which provides the basis for radiolabeling VIP as tumor diagnostic agent. However, fast proteolytic degradation of VIP i
- Cheng, Dengfeng,Yin, Duanzhi,Zhang, Lan,Wang, Mingwei,Li, Gucai,Wang, Yongxian
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- [18F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent
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Fluorine-18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine-18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain
- Zhang, Bo,Fraser, Benjamin H.,Klenner, Mitchell A.,Chen, Zhen,Liang, Steven H.,Massi, Massimiliano,Robinson, Andrea J.,Pascali, Giancarlo
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- Synthesis and liposome encapsulation of a novel 18F-conjugate of ω-conotoxin GVIA for the potential imaging of N-type Ca2+ channels in the brain by positron emission tomography
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ω-Conotoxin GVIA is a potent, irreversible antagonist of N-type voltage gated Ca2+ channels. A radiofluorinated analogue of GVIA could be useful in assessing regional synaptic density of the brain, in vivo, using positron emission tomography. N
- Azarian, Vahe,Gangloff, Anne,Seimbille, Yann,Delaloye, Sibylle,Czernin, Johannes,Phelps, Michael E.,Silverman, Daniel H. S.
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- Preliminary biological evaluation of 18F-FBEM-Cys-annexin V a novel apoptosis imaging agent
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A novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been developed and successfully labeled site-specifically with 18F-FBEM. 18F-FBEM was synthesized by coupling 18F-fluorobenzoic acid (18F-FBA) with N-(2-aminoethyl)maleimide using optimized reaction conditions. The yield of 18F-FBEM-Cys-Annexin V was 71.5% ± 2.0% (n = 4, based on the starting 18F-FBEM, non-decay corrected). The radiochemical purity of 18F-FBEM-Cys-Annexin V was >95%. The specific radioactivities of 18F-FBEM and 18F-FBEM-Cys-Annexin V were >150 and 3.17 GBq/μmol, respectively. Like the 1st generation 18F-SFB-Annexin V, the novel 18F-FBEM-Cys-Annexin V mainly shows renal and to a lesser extent, hepatobiliary excretion in normal mice. In rat hepatic apoptosis models a 3.88 ± 0.05 (n = 4, 1 h) and 10.35 ± 0.08 (n = 4, 2 h) increase in hepatic uptake of 18F-FBEM-Cys-Annexin V compared to normal rats was observed after injection via the tail vein. The liver uptake ratio (treated/control) at 2 h p.i. as measured via microPET correlated with the ratio of apoptotic nuclei in liver observed using TUNEL histochemistry, indicating that the novel 18F-FBEM-Cys-Annexin V is a potential apoptosis imaging agent.
- Lu, Chunxiong,Jiang, Quanfu,Hu, Minjin,Tan, Cheng,Yu, Huixin,Hua, Zichun
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- On-demand radiosynthesis of: N -succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) on an electrowetting-on-dielectric microfluidic chip for 18F-labeling of protein
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An all-electronic, droplet-based batch microfluidic device, operated using the electrowetting on dielectric (EWOD) mechanism was developed for on-demand synthesis of N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB), the most commonly
- Kim, Hee-Kwon,Javed, Muhammad Rashed,Chen, Supin,Zettlitz, Kirstin A.,Collins, Jeffrey,Wu, Anna M.,Kim, Chang-Jin,Michael Van Dam,Keng, Pei Yuin
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- Solid phase synthesis of [18F]labelled peptides for positron emission tomography
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A strategy for the solid phase synthesis of [18F]labelled peptides has been developed. The peptides were prepared on solid support and acylated with 4-[18F]fluorobenzoic acid using HATU within 3 min and the labelled peptide was relea
- Sutcliffe-Goulden, Julie L.,O'Doherty, Michael J.,Bansal, Sukhvinder S.
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- Identification, Characterization, and Optimization of Integrin αvβ6-Targeting Peptides from a One-Bead One-Compound (OBOC) Library: Towards the development of positron emission tomography (PET) imaging agents
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The current translation of peptides identified through the one-bead one-compound (OBOC) technology into positron emission tomography (PET) imaging agents is a slow process, with a major delay between ligand identification and subsequent lead optimization.
- Tang, Yng C.,Davis, Ryan A.,Ganguly, Tanushree,Sutcliffe, Julie L.
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- Fluorine-18 labeled galactosyl-neoglycoalbumin for imaging the hepatic asialoglycoprotein receptor
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Asialoglycoprotein receptors (ASGP-R) are well known to exist on the mammalian liver, situate on the surface of hepatocyte membrane. Quantitative imaging of asialoglycoprotein receptors could estimate the function of the liver. 99mTc labeled ga
- Yang, Wenjiang,Mou, Tiantian,Peng, Cheng,Wu, Zhanhong,Zhang, Xianzhong,Li, Fang,Ma, Yunchuan
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- NOVEL MOLECULAR ASSEMBLY, MOLECULAR PROBE FOR MOLECULAR IMAGING AND MOLECULAR PROBE FOR DRUG DELIVERY SYSTEM USING THE SAME, AND MOLECULAR IMAGING SYSTEM AND DRUG DELIVERY SYSTEM
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The present invention provides a molecular assembly which is less likely to accumulate in tissue other than cancer tissue, is highly safe for a living body, and can be prepared by a simple and safe method and whose particle size can be easily controlled.
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Paragraph 0547-0550
(2019/04/25)
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- Compound, composition, and method for detecting caspase activity and/or apoptosis
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Molecular probe suitable for quantification of caspase activity in vivo using positron emission tomography (PET). Embodiments of the present invention can detect apoptosis in tumors and as a novel, potentially translatable biomarker for predicting respons
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- Peptidomimetic growth hormone secretagogue derivatives for positron emission tomography imaging of the ghrelin receptor
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The ghrelin receptor is a seven-transmembrane (7-TM) receptor known to have an increased level of expression in human carcinoma and heart failure. Recent work has focused on the synthesis of positron emission tomography (PET) probes designed to target and image this receptor for disease diagnosis and staging. However, these probes have been restricted to small-molecule quinalizonones and peptide derivatives of the endogenous ligand ghrelin. We describe the design, synthesis and biological evaluation of a series of 4-fluorobenzoylated growth hormone secretagogues (GHSs) derived from peptidic (GHRP-1, GHPR-2 and GHRP-6) and peptidomimetic (G-7039, [1-Nal4]G-7039 and ipamorelin) families in order to test locations for the insertion of fluorine-18 for PET imaging. The peptidomimetic G-7039 was found to be the most suitable for 18F-radiolabelling as its non-radioactive 4-fluorobenzoylated analogue ([1-Nal4,Lys5(4-FB)]G-7039), had both a high binding affinity (IC50 = 69 nM) and promising in vitro efficacy (EC50 = 1.1 nM). Prosthetic group radiolabelling of the precursor compound [1-Nal4]G-7039 using N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) delivered the PET probe [1-Nal4,Lys5(4-[18F]-FB)]G-7039 in an average decay-corrected radiochemical yield of 48%, a radio-purity ≥ 99% and an average molar activity of >34 GBq/μmol. This compound could be investigated as a PET probe for the detection of diseases that are characterised by overexpression of the ghrelin receptor.
- Fowkes, Milan M.,Lalonde, Tyler,Yu, Lihai,Dhanvantari, Savita,Kovacs, Michael S.,Luyt, Leonard G.
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p. 1500 - 1511
(2018/09/18)
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- A recombinant human vascular endothelial chalone developer and its preparation method
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The invention relates to the technical field of recombinant human endostatin preparation prepared molecular targeting developers, and concretely provides a novel positron-emitting radionuclide or gadolinium labeled recombinant human endostatin developer a
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- PEPTIDOMIMETICS FOR IMAGING THE GHRELIN RECEPTOR
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ABSTRACT The present invention concerns compositions comprising and methods of identification and use of imaging agents. The imaging agents comprise a growth hormone secretagogues having a conjugated fluoride. The imaging agents of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease.
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- ANTI-MACROPHAGE MANNOSE RECEPTOR SINGLE VARIABLE DOMAINS FOR USE IN CARDIOVASCULAR DISEASES
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The disclosure relates to the field of cardiovascular diseases. In particular, immunoglobulin single variable domains directed against macrophage mannose receptor (MMR) are provided that can be used in the diagnosis, prognosis and/or monitoring of cardiov
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- 18F-LABELING OF AROMATIC AND HETEROAROMATIC MOLECULES WITH UNPROTECTED CARBOXYLIC ACID GROUPS
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The present invention provides a method for the 18F labeling of aromatic or heteroaromatic compounds containing an unprotected carboxylic acid group to yield labeled molecules which can be used as radiotracers. In addition, the invention provides precursor compounds containing an unprotected carboxylic acid group which can be used in such a method.
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Page/Page column 19-20
(2015/02/02)
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- A dual inhibitor of matrix metalloproteinases and a disintegrin and metalloproteinases, [18F]FB-ML5, as a molecular probe for non-invasive MMP/ADAM-targeted imaging
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Background Numerous clinical studies have shown a correlation between increased matrix metalloproteinase (MMP)/a disintegrin and metalloproteinase (ADAM) activity and poor outcome of cancer. Various MMP inhibitors (MMPIs) have been developed for therapeutic purposes in oncology. In addition, molecular imaging of MMP/ADAM levels in vivo would allow the diagnosis of tumors. We selected the dual inhibitor of MMPs and ADAMs, ML5, which is a hydroxamate-based inhibitor with affinities for many MMPs and ADAMs. ML5 was radiolabelled with 18F and the newly obtained radiolabelled inhibitor was evaluated in vitro and in vivo. Materials and methods ML5 was radiolabelled by direct acylation with N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB) for PET (positron emission tomography). The resulting radiotracer [18F]FB-ML5 was evaluated in vitro in human bronchial epithelium 16HBE cells and breast cancer MCF-7 cells. The non-radioactive probe FB-ML5 and native ML5 were tested in a fluorogenic inhibition assay against MMP-2, -9, -12 and ADAM-17. The in vivo kinetics of [18F]FB-ML5 were examined in a HT1080 tumor-bearing mouse model. Specificity of probe binding was examined by co-injection of 0 or 2.5 mg/kg ML5. Results ML5 and FB-ML5 showed high affinity for MMP-2, -9, -12 and ADAM-17; indeed IC50 values were respectively 7.4 ± 2.0, 19.5 ± 2.8, 2.0 ± 0.2 and 5.7 ± 2.2 nM and 12.5 ± 3.1, 31.5 ± 13.7, 138.0 ± 10.9 and 24.7 ± 2.8 nM. Radiochemical yield of HPLC-purified [18F]FB-ML5 was 13-16% (corrected for decay). Cellular binding of [18F]FB-ML5 was reduced by 36.6% and 27.5% in MCF-7 and 16HBE cells, respectively, after co-incubation with 10 μM of ML5. In microPET scans, HT1080 tumors exhibited a low and homogeneous uptake of the tracer. Tumors of mice injected with [18F]FB-ML5 showed a SUVmean of 0.145 ± 0.064 (n = 6) which decreased to 0.041 ± 0.027 (n = 6) after target blocking (p 18F. [18F]FB-ML5 demonstrated rather low binding in ADAM-17 overexpressing cell lines. [18F]FB-ML5 uptake showed significant reduction in the HT1080 tumor in vivo after co-injection of ML5. [18F]FB-ML5 may be suitable for the visualization/quantification of diseases overexpressing simultaneously MMPs and ADAMs.
- Matusiak, Nathalie,Castelli, Riccardo,Tuin, Adriaan W.,Overkleeft, Herman S.,Wisastra, Rosalina,Dekker, Frank J.,Prély, Laurette M.,Bischoff, Rainer P.M.,Van Waarde, Aren,Dierckx, Rudi A.J.O.,Elsinga, Philip H.
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p. 192 - 202
(2015/02/19)
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- Compound accumulating in inflammatory site, diagnostic agent containing the compound in labeled state and its precursor compound for labeling
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Embodiments of the invention provide a compound accumulating in an inflammatory site, a diagnostic agent containing the compound in labeled state and its precursor compound for labeling. Such a compound accumulating in inflammatory site may be represented
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- Fully automated synthesis and coupling of [18F]FBEM to glutathione using the iPHASE FlexLab module
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Site-specific radiolabelling of peptides or antibodies using [ 18F]FBEM is often preferred over non-site-specific radiolabelling with [18F]SFB because it does not affect the affinity of the antibody to its target. Unfortunately, the synthesis of [18F]FBEM and its conjugation to thiol containing macromolecules requires some manual intervention, which leads to radiation exposure of the radiochemist. In this publication, we report on the complete automation of [18F]FBEM production and its subsequent conjugation to glutathione using a slightly modified iPHASE FlexLab module. [18F]FBEM was produced in 1.185 ± 0.168 GBq (15-20%; n = 10; 0.75 ± 0.106 GBq non-decay corrected) with a specific activity of 57 ± 10 GBq/μmol. Radiochemical purity was 97 ± 1% and the synthesis time including HPLC purification and reformulation was 70 min. After evaporation to dryness, [18F]FBEM was conjugated to glutathione in PBS buffer pH 7.4 in quantitative yields. This fully automated method does not require any manual intervention and therefore reduces the radiation exposure to the operator. copy; 2014 John Wiley & Sons, Ltd.
- Ackermann, Uwe,Plougastel, Lucie,Wichmann, Christian,Goh, Yit Wooi,Yeoh, Shinn Dee,Poniger, Stan S.,Tochon-Danguy, Henri J.,Scott, Andrew M.
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p. 115 - 120
(2014/03/21)
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- FORMULATION OF RADIOPHARMACEUTICALS CONTAINING MULTIPLE ACIDIC GROUPS
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The invention relates to the subject matter referred to in the claims, i.e. surprisingly rapid and simple reformulation of very polar radiopharmaceuticals containing multiple acidic functional groups to solutions suitable for injecting into mammals.
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- METHOD OF SYNTHESIZING [18F]SFB USING MICROSYNTHESIS TECHNIQUE
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A method for synthesizing [18F]SFB is disclosed, which comprises using a microreactor including a substrate having one channel formed therein so as to have a cross-sectional width of 1 mm or less and a cross-sectional depth of 1 mm or less, the
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- Labeling approaches for the GE11 peptide, an epidermal growth factor receptor biomarker
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The epidermal growth factor receptor (EGFR) is involved in the proliferation and differentiation of normal and malignant cells and is a major therapeutic target for a variety of human cancers. The peptide GE11 was reported to bind efficiently to the EGFR.
- Dissoki, Samar,Hagooly, Aviv,Elmachily, Smadar,Mishani, Eyal
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p. 693 - 701
(2012/07/27)
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- Copper-free click for PET: Rapid 1,3-dipolar cycloadditions with a fluorine-18 cyclooctyne
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The strain-promoted click 1,3-dipolar cycloaddition reactions involving azides and cyclooctynes for the synthesis of triazoles offer the advantage of being able to be performed in biological settings via copper-free chemistries. While strained reagents conjugated to optical dyes and radiometal conjugates have been reported, cyclooctyne reagents labeled with fluorine-18 ( 18F) and radiochemically evaluated in a copper-free click reaction have yet to be explored. This report describes the conversion of a bifunctional azadibenzocyclooctyne (ADIBO) amine to the 18F-labeled cyclooctyne 4, the subsequent fast copper-free 1,3-dipolar cycloaddition reaction with alkyl azides at 37 °C (>70% radiochemical conversion in 30 min), and biological evaluations (serum stability of >95% at 2 h). These findings demonstrate the excellent reactivity of the 18F-labeled cyclooctyne 4 with readily available azides that will allow future work focusing on rapid copper-free in vitro and in vivo click chemistries for PET imaging using 18F-labeled cyclooctyne derivatives of ADIBO.
- Carpenter, Richard D.,Hausner, Sven H.,Sutcliffe, Julie L.
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p. 885 - 889
(2012/02/01)
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- Synthesis of 2-[(4-[18F]Fluorobenzoyloxy)methyl]-1,4- naphthalenedione from 2-hydroxymethyl 1,4-naphthoquinone and 4-[ 18F]fluorobenzoic acid using dicyclohexyl carbodiimide
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2-[(4-[18F]Fluorobenzoyloxy)methyl]-1,4-naphthalenedione ([ 18F]1) was synthesised as a putative hypoxia imaging agent from 2-hydroxymethyl 1,4-naphthoquinone (7) and 4-[18F]fluorobenzoic acid ([18F]8) using dicyclohexyl carbodiimide (DCC) to activate [ 18F]8. This coupling reaction was fast and gave quantitative yields. Further investigations are warranted on the use of DCC as a coupling agent in Positron Emission Tomography. The synthesis including HPLC purification and reformulation has been fully automated on a modified FDG synthesiser with two reactor vials. [18F]1 was produced in a radiochemical yield of 27 ± 5%, with a radiochemical purity of 97.5% and a specific activity of 78.4-134.5 GBq/μmol at the end of synthesis (n = 23). The total synthesis time including reformulation was 65 min. [18F]1 was found to be stable in plasma and saline, but underwent rapid metabolism in a phase 1 metabolite assay using rat S9 liver fractions. An in vivo evaluation of [ 18F]1 in transplanted, hypoxic SK-RC-52 tumour-bearing BALB/c nude mice revealed the tumour-to-muscle ratio to be 2.4 ± 0.1 at 2 h post-injection.
- Ackermann, Uwe,Sigmund, Duanne,Yeoh, Shinn Dee,Rigopoulos, Angela,O'Keefe, Graeme,Cartwright, Glenn,White, Jonathan,Scott, Andrew M.,Tochon-Danguy, Henri J.
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p. 788 - 794
(2012/05/20)
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- Radiosynthesis and in vivo evaluation of a F-18-labeled pancreatic islet amyloid inhibitor
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Formation of islet amyloid deposits contributes to the progressive loss of beta-cells in Type 2 diabetes. Islet amyloid is composed of islet amyloid polypeptide (IAPP). [(N-Me)G24, (N-Me)I26]hIAPP(22-27) peptide was found to bind hum
- Pathuri, Gopal,Agashe, Hrushikesh B.,Awasthi, Vibhudutta,Gali, Hariprasad
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experimental part
p. 186 - 191
(2011/08/06)
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- Orthogonal 18F and 64Cu labelling of functionalised bis(thiosemicarbazonato) complexes
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The synthesis of three pairs of orthogonally labelled fluorinated Cu bis(thiosemicarbazonato) complexes is presented. These are the first examples of 18F-labelled Cu(ii)-complexes designed to serve as new hypoxia selective PET tracers and as mechanistic probes to study the mode of action of this class of markers. In vitro evaluation revealed that the fluorinated Cu-complex derived from amide coupling is suitable for in vivo work.
- Carroll, Laurence,Bejot, Romain,Hueting, Rebekka,King, Robert,Bonnitcha, Paul,Bayly, Simon,Christlieb, Martin,Dilworth, Jonathan R.,Gee, Antony D.,Declerck, Jerome,Gouverneur, Veronique
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scheme or table
p. 4052 - 4054
(2010/09/06)
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- RADIOLABELED AFFIBODY MOLECULES
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The invention provides a radiolabeled affibody molecule comprising a fragment of an IgG-binding domain of protein A from Staphylococcus aureus, a bifunctional linker, and a radiolabel comprising 18F or 76Br, wherein the bifunctional
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Page/Page column 16-17
(2008/12/04)
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- Synthesis of a potent and selective 18F-labeled δ-opioid receptor antagonist derived from the Dmt-Tic pharmacophore for positron emission tomography imaging
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Identification and pharmacological characterization of two new selective δ-opioid receptor antagonists, derived from the Dmt-Tic pharmacophore, of potential utility in positron emission tomography (PET) imaging are described. On the basis of its high δ se
- Eun, Kyoung Ryu,Wu, Zhanhong,Chen, Kai,Lazarus, Lawrence H.,Marczak, Ewa D.,Sasaki, Yusuke,Ambo, Akihiro,Salvadori, Severo,Ren, Chuancheng,Zhao, Heng,Balboni, Gianfranco,Chen, Xiaoyuan
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p. 1817 - 1823
(2008/12/20)
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- Novel synthesis of [18F]-fluorobenzene and pyridinecarbohydrazide-folates as potential PET radiopharmaceuticals
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In an attempt to visualize folate receptors that over-express on many cancers, [18F]-fluorobenzene and pyridine carbohydrazide-folates were synthesized using two different synthetic approaches starting from nucleophilic displacement reactions on ethyl-trimethylammonium-benzoate and pyridine carboxylate precursors. The intermediates ethyl [18F]-fluorinated benzene and pyridine esters were reacted with hydrazine to produce the [ 18F]-fluorobenzene and pyridine carbohydrazides followed by coupling with NHS-folate 11 in the first approach. Whereas hydrazide-folate 5 was reacted with 2,5-dioxoazolidinyl [18F]-fluorobenzenecarboxylate in the second approach. Based on starting [18F]-fluoride, radiochemical yields and synthesis times were found to be around 80% (45 min) and 35% (80 min) for the first and the second approaches, respectively. The first synthetic approach holds considerable promise as a rapid and simple method for the radiofluorination of folic acid with high radiochemical yield and short time. Copyright
- Al Jammaz,Al-Otaibi,Okarvi,Amartey
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p. 125 - 137
(2007/10/03)
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- Synthesis of an18F-fluorobenzoate idarubicin derivative as new potential PET radiotracer to predict chemotherapy resistance
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Anthracyclines are among the most widely used antineoplastic agents in current clinical practice. Nevertheless, chemoresistance, which results in failure to eradicate the tumor, is often observed after administration of anthracyclines, and no assay system
- Seimbille, Yann,Czernin, Johannes,Phelps, Michael E.,Silverman, Daniel H. S.
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p. 819 - 827
(2007/10/03)
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- Radiolabeling of unprotected octreotide with F-18
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Octreotide can be labeled with fluorine-18 as a potential radiopharmaceutical for quantitative in vivo mapping of somatostatin receptors incancer patients. A one step synthesis that does not involve blocking and unblocking of the ε-lysine amine would prev
- Panico, M.,Lang, L.,Sassaman, M. B.,Eckelman, W. C.
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p. S922 - S924
(2007/10/03)
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- Development of fluorine-18-labeled 5-HT(1A) antagonists
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We have synthesized five fluorinated derivatives of WAY 100635, N-{2- [4-(2-methoxyphenyl)piperazino]ethyl)-N-(2-pyridyl)cyclohexanecarboxamide (4a), using various acids in place of the cyclohexanecarboxylic acid (CHCA, 2a) in the reaction scheme. The five acids are 4-fluorobenzoic acid (FB, 2b), 4-fluoro-3-methylbenzoic acid (MeFB, 2c), trans-4- fluorocyclohexanecarboxylic acid (FC, 2d), 4-(fluoromethyl)benzoic acid (FMeB, 2e), and 3-nitro-4(fluoromethyl)benzoic acid (NFMeB, 2f) (see Scheme 1). These compounds were radiolabeled with fluorine-18, and their biological properties were evaluated in rats and compared with those of [11C]carbonyl WAY 100635 ([carbonyl-11C]4a). [Carbonyl-11C]4a cleared the brain with a biological half-life averaging 41 min. The metabolite-corrected blood radioactivity had a half-life of 29 min. [18F]FCWAY ([18F]4d) gave half- lives and intercepts comparable to [carbonyl11C]4a in the brain, but the blood clearance was faster. [18F]FBWAY ([18F]4b) showed an early rapid net efflux from the whole brain, clearing with a biological half-life of 35 min. The metabolite-corrected blood half-life was 41 min. The comparable whole brain and blood half-lives for Me[18F]FBWAY ([18F]4c) were 16 and 18 min, respectively. For each compound, the corresponding carboxylic acid was identified as a major metabolite in blood. Fluoride was also found after injection of [18F]4d. However, for all compounds there was a good correlation (R > 0.97) between the differential uptake ratio (DUR, (%ID/g) x body weight (g)/100) in individual rat brain regions at 30 min after injection and the concentration of receptors as determined by in vitro quantitative autoradiography in rat. Specific binding ratios [region of interest (ROI)/cerebellum-1] in control studies for cortex (Ctx) and hippocampus (H) were higher for [carbonyl11C]4a and [18F]4d compared to [18F]4b and [18F]4c. [18F]4d has similar pharmacokinetic properties and comparable specific binding ratios to [carbonyl-11C]4a. Fifty nanomoles of 4a blocked only 30% of the specific binding of [18F]4d, while complete blockade was obtained from co-injection of 200 nmol of 4a (H/Cb-1 from 17.2 to 0.6). [18F]4b and [18F]4c showed lower specific binding ratios than [carbonyl-11C]4a and [18F]4d. [18F]4c was superior to [18F]4b since its specific binding was more readily blocked by 4a. These studies suggest that [18F]4c should be a useful compound to assess dynamic changes in serotonin levels while [18F]4d, with its high contrast and F-18 label, should provide better statistics and quantification for static measurement of 5-HT(1A) receptor distribution.
- Lang, Lixin,Jagoda, Elaine,Schmall, Bernard,Vuong, Bik-Kee,Adams, H. Richard,Nelson, David L.,Carson, Richard E.,Eckelman, William C.
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p. 1576 - 1586
(2007/10/03)
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- 18F-labelling of oligonucleotides using succinimido 4-[18F]fluorobenzoate
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A general method for the labelling of oligodeoxynucleotides and oligonucleoside phosphorothioates in the 5′-position with the positron-emitting radionuclide 18F (t1/2=110 min) is described. The label was incorporated by the reaction
- Hedberg, Elisabeth,Langstroem, Bengt
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p. 1034 - 1039
(2007/10/03)
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