当前位置： SCI文献检索 > MOLECULAR IMAGING AND BIOLOGY期刊下所有文献 > Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems.

Predicting the success of a radiopharmaceutical for in vivo imaging of central nervous system neuroreceptor systems.

Abstract：

:In vivo imaging of the central nervous system (CNS) neuroreceptors in humans began was used in the early 1980s. Now, some twenty years later, the success of radiopharmaceutical imaging is still often one based on empiricism and serendipity. Nevertheless, a number of factors can be identified based on the robot experience in developing these radiotracers. This article will describe some of the issues that may be useful in choosing approaches to radiolabel ligands as future imaging agents of neuroreceptors, transporters and intrasynaptic measures of neurotransmitters. A description of the current process from hypothesis to radiochemical preclinical development, non-human primate imaging development of quantitative procedures finally leading to toxicology, dosimetry and eventually human applications are provided. The role of important factors including metabolism and lipophilicity, affinity and other factors for optimizing radiolabeling strategies is dealt with. Furthermore, issues involving decision making of how far to extend efforts in developing a radiotracer and when might be an appropriate stopping place are discussed. Finally some typical examples of the use of these radiotracers, especially with emphasis on stable drug design and development, are provided. These include occupancy studies and mechanism of action studies. In summary, the prediction of tracer success includes: first, identification of appropriate targets and precursors, then systematic optimization of ligands with continuous feedback from pharmacokinetics and iterative improvement based on unsuccessful tracers. This article is intended to present a pragmatic overview of the radiopharmaceutical development process with emphasis on the CNS.

journal_name

Mol Imaging Biol

journal_title

Molecular imaging and biology

authors

Wong DF,Pomper MG

doi

10.1016/j.mibio.2003.09.011

keywords:

subject

Has Abstract

pub_date

2003-11-01 00:00:00

pages

350-62

issue

6

eissn

1536-1632

issn

1860-2002

pii

S1536163203001690

journal_volume

5

pub_type

杂志文章,评审

相关文献

MOLECULAR IMAGING AND BIOLOGY文献大全
  • SUV95th as a Reliable Alternative to SUVmax for Determining Renal Uptake in [68Ga] PSMA PET/CT.

    abstract：PURPOSE:Widely used in clinical practice, the maximum standardized uptake value (SUVmax) is a statistical index highly prone to physical and biological variations, which can lead to unpredictable errors. This study has a methodological aim: to identify a more robust SUV-based index representing the tracer accumulation....

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-019-01451-1

    authors： Baiocco S,Matteucci F,Mezzenga E,Caroli P,Di Iorio V,Cittanti C,Bevilacqua A,Paganelli G,Sarnelli A

    更新日期：2020-08-01 00:00:00

  • SPECT Imaging of Muscle Injury with [99mTc]MDP in a Mouse Model of Muscular Dystrophy.

    abstract：PURPOSE:Tc-99m methylene diphosphonate ([99mTc]MDP) is an in vivo bone imaging agent that also accumulates in injured skeletal muscle cells. The objective of this study was to investigate if [99mTc]MDP could be used to detect muscle injury in the mdx mouse model of Duchenne muscular dystrophy (DMD). PROCEDURES:Static ...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-019-01394-7

    authors： Gaut C,Sullivan JM,Biscaro B,Soares EJ,Nicholson K,Hoppin J,Verma A

    更新日期：2020-06-01 00:00:00

  • Integrin α(v)β₃ as a PET imaging biomarker for osteoclast number in mouse models of negative and positive osteoclast regulation.

    abstract：PURPOSE:The goal of this study was to determine the specificity of ⁶⁴Cu-CB-TE2A-c(RGDyK) (⁶⁴Cu-RGD) for osteoclast-related diseases, such as Paget's disease or rheumatoid arthritis. PROCEDURES:C57BL/6 mice were treated systemically with osteoprotegerin (OPG) for 15 days or RANKL for 11 days to suppress and stimulate o...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-011-0512-4

    authors： Zheleznyak A,Wadas TJ,Sherman CD,Wilson JM,Kostenuik PJ,Weilbaecher KN,Anderson CJ

    更新日期：2012-08-01 00:00:00

  • Tracking long-term survival of intramyocardially delivered human adipose tissue-derived stem cells using bioluminescence imaging.

    abstract：PURPOSE:Transplantation of a regenerative cell population derived from human subcutaneous adipose tissue (hASCs) for cardiac regeneration represents a promising therapy due to the capacity of these cells for proliferation and differentiation. Understanding the fate of injected hASCs would help to understand how hASCs w...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-010-0392-z

    authors： Bai X,Yan Y,Coleman M,Wu G,Rabinovich B,Seidensticker M,Alt E

    更新日期：2011-08-01 00:00:00

  • Reproducibility of non-invasive a1 adenosine receptor quantification in the rat brain using [(18)F]CPFPX and positron emission tomography.

    abstract：PURPOSE:The A1AR antagonist 8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine ([(18)F]CPFPX) has recently been shown to be a suitable radiotracer for quantitative in vivo imaging of the A1 adenosine receptor (A1AR) in rats. The present study evaluates the reproducibility of non-invasive longitudinal A1AR studies with [...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-014-0729-0

    authors： Kroll T,Elmenhorst D,Weisshaupt A,Beer S,Bauer A

    更新日期：2014-10-01 00:00:00

  • Standardized Uptake Values in 2-Deoxy-2-[18F]Fluoro-D-Glucose with Positron Emission Tomography. Clinical Significance of Iterative Reconstruction and Segmented Attenuation Compared with Conventional Filtered Back Projection and Measured Attenuation Corre

    abstract：PURPOSE:To evaluate the clinical significance of differences in 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography (FDG-PET) lymph node standardized uptake values (SUV) in human immunodeficiency virus (HIV) infection using iterative reconstruction with segmented attenuation correction (IR SAC) compared to fil...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1016/s1536-1632(02)00014-8

    authors： Chin BB,Lyengar S,Sabundayo BP,Schwartz D

    更新日期：2002-07-01 00:00:00

  • Imaging of Tumor Spheroids, Dual-Isotope SPECT, and Autoradiographic Analysis to Assess the Tumor Uptake and Distribution of Different Nanobodies.

    abstract：PURPOSE:Recent studies have shown rapid accumulation of nanobodies (NBs) in tumors and fast clearance of the unbound fraction, making NBs exceptional tracers for cancer imaging. In this study, we investigate the combination of in vitro imaging of tumor spheroids, in vivo dual-isotope single-photon emission computed tom...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-019-01320-x

    authors： Beltrán Hernández I,Rompen R,Rossin R,Xenaki KT,Katrukha EA,Nicolay K,van Bergen En Henegouwen P,Grüll H,Oliveira S

    更新日期：2019-12-01 00:00:00

  • Development of antibody-carrying microbubbles based on clinically available ultrasound contrast agent for targeted molecular imaging: a preliminary chemical study.

    abstract：PURPOSE:The purpose of the study was to examine the feasibility of an antibody-carrying targeted-bubble preparation using clinically available phosphatidylserine (PS)-containing perfluorobutane-filled microbubbles for molecular ultrasound imaging. PROCEDURES:Firstly, we examined whether PS on the surface of perfluorob...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-010-0344-7

    authors： Otani K,Yamahara K

    更新日期：2011-04-01 00:00:00

  • Molecular Imaging of PDE10A Knockout Mice with a Novel PET Radiotracer: [(11)C]T-773.

    abstract：PURPOSE:[(11)C]T-773 is a new radioligand for positron emission tomography (PET) targeting the phosphodiesterase 10A enzyme (PDE10A). PDE10A is highly expressed in the striatum by medium spiny neurons, and it has been demonstrated to be involved in the regulation of striatal signaling through the reduction of medium sp...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-015-0822-z

    authors： Tóth M,Häggkvist J,Stepanov V,Takano A,Nakao R,Amini N,Miura S,Kimura H,Taniguchi T,Gulyás B,Halldin C

    更新日期：2015-08-01 00:00:00

  • Articulated whole-body atlases for small animal image analysis: construction and applications.

    abstract：PURPOSE:Using three publicly available small-animal atlases (Sprague-Dawley rat, MOBY, and Digimouse), we built three articulated atlases and present several applications in the scope of molecular imaging. PROCEDURES:Major bones/bone groups were manually segmented for each atlas skeleton. Then, a kinematic model for e...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-010-0386-x

    authors： Khmelinskii A,Baiker M,Kaijzel EL,Chen J,Reiber JH,Lelieveldt BP

    更新日期：2011-10-01 00:00:00

  • Impact of FDG-PET on prediction of clinical outcome after concurrent chemoradiotherapy in hypopharyngeal carcinoma.

    abstract：PURPOSE:To evaluate prognostic value of pretreatment and posttreatment 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography (FDG-PET) in advanced hypopharyngeal carcinoma treated by chemoradiotherapy. PROCEDURES:Thirty-one patients underwent a baseline FDG-PET and then FDG-PET was repeated 7 weeks after chemor...

    journal_title：Molecular imaging and biology

    pub_type： 临床试验,杂志文章

    doi：10.1007/s11307-009-0229-9

    authors： Inohara H,Enomoto K,Tomiyama Y,Higuchi I,Inoue T,Hatazawa J

    更新日期：2010-01-01 00:00:00

  • Impact of 2-deoxy-2[F-18]fluoro-D-glucose Positron Emission Tomography on the management of patients with advanced melanoma.

    abstract：OBJECTIVES:Accurate staging of patients with melanoma is vital to guide appropriate treatment. 2-Deoxy-2-[F-18]fluoro-D-glucose (FDG)-positron emission tomography (PET) has been reported to be a sensitive and specific technique for the staging of advanced melanoma, however, few studies provide information regarding its...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-005-0002-7

    authors： Harris MT,Berlangieri SU,Cebon JS,Davis ID,Scott AM

    更新日期：2005-07-01 00:00:00

  • The effect of insulin on the intracellular distribution of 14(R,S)-[18F]Fluoro-6-thia-heptadecanoic acid in rats.

    abstract：PURPOSE:The aim of this study was to determine the effect of hyperinsulinemia on myocardial and hepatic distribution and metabolism of 14(R,S)-[18F]fluoro-6-thia-heptadecanoic acid ([18F]FTHA). PROCEDURES:Mitochondrial retention and intracellular lipid incorporation of [18F]FTHA were compared to that of [14C]-2-bromop...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-006-0042-7

    authors： Ci X,Frisch F,Lavoie F,Germain P,Lecomte R,van Lier JE,Bénard F,Carpentier AC

    更新日期：2006-07-01 00:00:00

  • High vascular delivery of EGF, but low receptor binding rate is observed in AsPC-1 tumors as compared to normal pancreas.

    abstract：PURPOSE:Cellular receptor targeted imaging agents present the potential to target extracellular molecular expression in cancerous lesions; however, the image contrast in vivo does not reflect the magnitude of overexpression expected from in vitro data. Here, the in vivo delivery and binding kinetics of epidermal growth...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-011-0503-5

    authors： Samkoe KS,Sexton K,Tichauer KM,Hextrum SK,Pardesi O,Davis SC,O'Hara JA,Hoopes PJ,Hasan T,Pogue BW

    更新日期：2012-08-01 00:00:00

  • Conditional bicistronic Cre reporter line expressing both firefly luciferase and β-galactosidase.

    abstract：PURPOSE:The Cre-loxP system has become an important strategy for conditional gene deletion and conditional gene expression in genetically engineered mice. To evaluate Cre recombinase expression, we generated reporter mice that permit both noninvasive imaging in living animals and either ex vivo histochemical/immunohist...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-010-0333-x

    authors： Ishikawa TO,Herschman HR

    更新日期：2011-04-01 00:00:00

  • Evaluation of 89Zr-rituximab tracer by Cerenkov luminescence imaging and correlation with PET in a humanized transgenic mouse model to image NHL.

    abstract：PURPOSE:This research aimed to study the use of Cerenkov luminescence imaging (CLI) for non-Hodgkin's lymphoma (NHL) using 89Zr-rituximab positron emission tomography (PET) tracer with a humanized transgenic mouse model that expresses human CD20 and the correlation of CLI with PET. PROCEDURES:Zr-rituximab (2.6 MBq) wa...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-013-0624-0

    authors： Natarajan A,Habte F,Liu H,Sathirachinda A,Hu X,Cheng Z,Nagamine CM,Gambhir SS

    更新日期：2013-08-01 00:00:00

  • Targeting gelatinases with a near-infrared fluorescent cyclic His-Try-Gly-Phe peptide.

    abstract：PURPOSE:The purpose of the study is to synthesize and characterize near-infrared (NIR) fluorescence imaging probes targeted to gelatinases. PROCEDURES:A phage display-selected cyclic peptide containing the His-Try-Gly-Phe (HWGF) motif was used as the lead compound. Structure-activity relationship analysis was used to ...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-009-0219-y

    authors： Wang W,Shao R,Wu Q,Ke S,McMurray J,Lang FF Jr,Charnsangavej C,Gelovani JG,Li C

    更新日期：2009-11-01 00:00:00

  • Histogram Analysis of T1-Weighted, T2-Weighted, and Postcontrast T1-Weighted Images in Primary CNS Lymphoma: Correlations with Histopathological Findings-a Preliminary Study.

    abstract：PURPOSE:Previously, some reports mentioned that magnetic resonance imaging (MRI) can predict histopathological features in primary CNS lymphoma (PCNSL). The reported data analyzed diffusion-weighted imaging findings. The aim of this study was to investigate possible associations between histopathological findings, such...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-017-1115-5

    authors： Meyer HJ,Schob S,Münch B,Frydrychowicz C,Garnov N,Quäschling U,Hoffmann KT,Surov A

    更新日期：2018-04-01 00:00:00

  • Coregistration of magnetic resonance and single photon emission computed tomography images for noninvasive localization of stem cells grafted in the infarcted rat myocardium.

    abstract：:This paper demonstrates the application of mutual information based coregistration of radionuclide and magnetic resonance imaging (MRI) in an effort to use multimodality imaging for noninvasive localization of stem cells grafted in the infarcted myocardium in rats. Radionuclide imaging such as single photon emission c...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-006-0062-3

    authors： Shen D,Liu D,Cao Z,Acton PD,Zhou R

    更新日期：2007-01-01 00:00:00

  • (18)F-FDG PET/CT imaging detects therapy efficacy of anti-EMMPRIN antibody and gemcitabine in orthotopic pancreatic tumor xenografts.

    abstract：PURPOSE:The objective of this study is to evaluate the therapeutic response to a novel monoclonal antibody targeting human extracellular matrix metalloproteinase inducer (EMMPRIN) in combination with gemcitabine in a pancreatic-tumor xenograft murine model by sequential 2-deoxy-2-[18F]fluoro-D-glucose ((18)F-FDG) posit...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-011-0491-5

    authors： Shah N,Zhai G,Knowles JA,Stockard CR,Grizzle WE,Fineberg N,Zhou T,Zinn KR,Rosenthal EL,Kim H

    更新日期：2012-04-01 00:00:00

  • Use of positron emission tomography to target prostate cancer gene therapy by oncolytic herpes simplex virus.

    abstract：:Herpes simplex virus (HSV) oncolytic gene therapy is a promising treatment modality against cancer. We have demonstrated that androgen-induced cellular changes enhance oncolytic viral replication and improve efficacy in the treatment of androgen-dependent prostate cancer cell line. Imaging of changes in 2-deoxy-2-[F-1...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-005-0028-x

    authors： Mullerad M,Eisenberg DP,Akhurst TJ,Adusumilli PS,Riedl CC,Bhargava A,Gonen M,Finn R,Scardino PT,Fong Y

    更新日期：2006-01-01 00:00:00

  • Evaluation of [99mTc]Radiolabeled Macrophage Mannose Receptor-Specific Nanobodies for Targeting of Atherosclerotic Lesions in Mice.

    abstract：PURPOSE:Macrophage accumulation characterizes the development of atherosclerotic plaques, and the presence of certain macrophage subsets might be an indicator of plaque phenotype and (in)stability. The macrophage mannose receptor (MMR) is expressed on alternatively activated macrophages and found at sites of intraplaqu...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-017-1117-3

    authors： Bala G,Baudhuin H,Remory I,Gillis K,Debie P,Krasniqi A,Lahoutte T,Raes G,Devoogdt N,Cosyns B,Hernot S

    更新日期：2018-04-01 00:00:00

  • ImmunoPET Imaging of αvβ6 Expression Using an Engineered Anti-αvβ6 Cys-diabody Site-Specifically Radiolabeled with Cu-64: Considerations for Optimal Imaging with Antibody Fragments.

    abstract：PURPOSE:Increased expression of the αvβ6 integrin correlates with advanced tumor grade and poor clinical outcome, identifying αvβ6 as a prognostic indicator and an attractive target for molecular imaging. This work investigated the ability of a disulfide-stabilized [64Cu]NOTA-αvβ6 cys-diabody to image αvβ6 expression i...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-017-1097-3

    authors： White JB,Hu LY,Boucher DL,Sutcliffe JL

    更新日期：2018-02-01 00:00:00

  • A comparison between time domain and spectral imaging systems for imaging quantum dots in small living animals.

    abstract：PURPOSE:We quantified the performance of time-domain imaging (TDI) and spectral imaging (SI) for fluorescence imaging of quantum dots (QDs) in three distinct imaging instruments: eXplore Optix (TDI, Advanced Research Technologies Inc.), Maestro (SI, CRi Inc.), and IVIS-Spectrum (SI, Caliper Life Sciences Inc.). PROCED...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-009-0290-4

    authors： de la Zerda A,Bodapati S,Teed R,Schipper ML,Keren S,Smith BR,Ng JS,Gambhir SS

    更新日期：2010-10-01 00:00:00

  • Whole body biodistribution and radiation dosimetry in humans of a new PET ligand, [(18)F]-FEPPA, to image translocator protein (18 kDa).

    abstract：PURPOSE:[(18)F]-FEPPA is a translocator protein (18 kDa, TSPO) positron emission tomography (PET) radiotracer. Radiation dosimetry was estimated from the whole body biodistribution, taking into consideration TSPO rs6971 (Ala147Thr) polymorphism. PROCEDURES:[(18)F]-FEPPA whole body PET scans were acquired for six healt...

    journal_title：Molecular imaging and biology

    pub_type： 临床试验,杂志文章

    doi：10.1007/s11307-012-0589-4

    authors： Mizrahi R,Rusjan PM,Vitcu I,Ng A,Wilson AA,Houle S,Bloomfield PM

    更新日期：2013-06-01 00:00:00

  • Lectin-Gd-loaded chitosan hydrogel nanoparticles: a new biospecific contrast agent for MRI.

    abstract：PURPOSE:Non-specific extracellular contrast agents have been on the market for more than 15 years. Here, we report on the synthesis of new selective lectin-gadolinium (Gd)-loaded chitosan nanoparticles with a prolonged clearance time and a much higher relaxivity in comparison to other preparations. PROCEDURES:Chitosan...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-010-0309-x

    authors： Pashkunova-Martic I,Kremser C,Galanski M,Arion V,Debbage P,Jaschke W,Keppler B

    更新日期：2011-02-01 00:00:00

  • The EIIAPA chimeric promoter for tumor specific gene therapy of hepatoma.

    abstract：PURPOSE:For targeted imaging and therapy of hepatocellular carcinoma (HCC), we established a chimeric promoter (EIIAPA) containing alpha-fetoprotein (AFP) promoter and hepatitis B virus enhancer II (EIIA) to control downstream expression of reporter and therapeutic genes. PROCEDURES:We combined AFP promoter and EIIA t...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-011-0509-z

    authors： Hsieh YJ,Chen FD,Ke CC,Wang HE,Huang CJ,Hou MF,Lin KP,Gelovani JG,Liu RS

    更新日期：2012-08-01 00:00:00

  • Correction to: The 2019 World Molecular Imaging Congress (WMIC) and Molecular Imaging and Biology (MIB) Awards.

    abstract：:The Commercial Innovation of the Year Award went to Emile Beaulieu of Photon etc. for their work. ...

    journal_title：Molecular imaging and biology

    pub_type： 已发布勘误

    doi：10.1007/s11307-019-01457-9

    authors： Lewis JS,Membreno R

    更新日期：2020-02-01 00:00:00

  • [123I]Metaiodobenzylguanidine (MIBG) Cardiac Scintigraphy and Automated Classification Techniques in Parkinsonian Disorders.

    abstract：PURPOSE:To provide reliable and reproducible heart/mediastinum (H/M) ratio cut-off values for parkinsonian disorders using two machine learning techniques, Support Vector Machines (SVM) and Random Forest (RF) classifier, applied to [123I]MIBG cardiac scintigraphy. PROCEDURES:We studied 85 subjects, 50 with idiopathic ...

    journal_title：Molecular imaging and biology

    pub_type： 杂志文章

    doi：10.1007/s11307-019-01406-6

    authors： Nuvoli S,Spanu A,Fravolini ML,Bianconi F,Cascianelli S,Madeddu G,Palumbo B

    更新日期：2020-06-01 00:00:00

  • Biodistribution and Radiation Dosimetry of [18F]Mefway in Humans.

    abstract：PURPOSE:[18F]Mefway is a positron emission tomography (PET) radioligand for quantification of the brain serotonin 1A (5-HT1A) receptor density. The purpose of this study was to evaluate the radiation safety of [18F]Mefway in humans. PROCEDURES:Six healthy volunteers (three males and three females) were whole-body PET ...

    journal_title：Molecular imaging and biology

    pub_type： 临床试验,杂志文章

    doi：10.1007/s11307-016-0955-8

    authors： Choi JY,Lyoo CH,Kim JS,Kim KM,Lee M,Ryu YH

    更新日期：2016-12-01 00:00:00