当前位置： SCI文献检索 > NUCLEAR MEDICINE AND BIOLOGY期刊下所有文献 > Biodistribution studies of two 18F-labeled pyridinylphenyl amides as subtype selective radioligands for the dopamine D3 receptor.

Biodistribution studies of two 18F-labeled pyridinylphenyl amides as subtype selective radioligands for the dopamine D3 receptor.

Abstract：

INTRODUCTION:Dopamine D3 receptors are implicated in various neuropsychiatric diseases, drug abuse and alcoholism, but specific agents for D3 molecular imaging are lacking. We evaluated two in vitro selective fluorine-18-labeled radioligand candidates ([(18)F]5 and [(18)F]6) for positron emission tomography (PET) imaging of D3 receptor availability in the brain. METHODS:Biodistribution was evaluated in Sprague-Dawley rats using ex vivo autoradiography and small-animal PET. Protein binding studies were conducted in human plasma and cerebrospinal fluid. RESULTS:[(18)F]5 showed rapid blood-brain barrier penetration and fast washout after intravenous injection, whereas the rat brain penetration of [(18)F]6 was lower. The total distribution volume (VT) of [(18)F]5 was 20-26 mL g(-1) throughout brain. Co-injection with the D3 antagonist BP897 resulted in globally increased cerebral washout of [(18)F]5 and [(18)F]6, but SUV analysis and parametric mapping of binding potential (BPND) relative to the cerebellum did not reveal specific binding of either ligand in D3-rich brain regions, i.e. the ventral striatum. However, there was substantial displaceable binding of [(18)F]5, and to a lesser extent [(18)F]6, in the pituitary. CONCLUSION:These radioligands reveal dopamine D3 receptors in the pituitary, but are not suitable for PET imaging of in brain, possibly due to low specific signal relative to the globally high VT.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Hocke C,Cumming P,Maschauer S,Kuwert T,Gmeiner P,Prante O

doi

10.1016/j.nucmedbio.2013.12.014

subject

Has Abstract

pub_date

2014-03-01 00:00:00

pages

223-8

issue

3

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(13)00262-X

journal_volume

41

pub_type

杂志文章

相关文献

NUCLEAR MEDICINE AND BIOLOGY文献大全
  • Radiosynthesis, biodistribution and imaging of [11C]YM155, a novel survivin suppressant, in a human prostate tumor-xenograft mouse model.

    abstract：INTRODUCTION:Sepantronium bromide (YM155) is an antitumor drug in development and is a first-in-class chemical entity, which is a survivin suppressant. We developed a radiosynthesis of [(11)C]YM155 to non-invasively evaluate its tissue and tumor distribution in mice bearing human prostate tumor xenografts. METHODS:Met...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2012.10.002

    authors： Murakami Y,Matsuya T,Kita A,Yamanaka K,Noda A,Mitsuoka K,Nakahara T,Miyoshi S,Nishimura S

    更新日期：2013-02-01 00:00:00

  • [(68)Ga]FSC-(RGD)3 a trimeric RGD peptide for imaging αvβ3 integrin expression based on a novel siderophore derived chelating scaffold-synthesis and evaluation.

    abstract：:Over the last years Gallium-68 ((68)Ga) has received tremendous attention for labeling of radiopharmaceuticals for positron emission tomography (PET). (68)Ga labeling of biomolecules is currently based on bifunctional chelators containing aminocarboxylates (mainly DOTA and NOTA). We have recently shown that cyclic pep...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2014.10.001

    authors： Knetsch PA,Zhai C,Rangger C,Blatzer M,Haas H,Kaeopookum P,Haubner R,Decristoforo C

    更新日期：2015-02-01 00:00:00

  • Efficient automated one-step synthesis of 2-[18F]fluoroethylcholine for clinical imaging: optimized reaction conditions and improved quality controls of different synthetic approaches.

    abstract：UNLABELLED:[(18)F]-labelled choline analogues, such as 2-[(18)F]fluoroethylcholine ((18)FECH), have suggested to be a new class of choline derivatives highly useful for the imaging of prostate and brain tumours. In fact, tumour cells with enhanced proliferation rate usually exhibit an improved choline uptake due to the...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2009.12.009

    authors： Asti M,Farioli D,Iori M,Guidotti C,Versari A,Salvo D

    更新日期：2010-04-01 00:00:00

  • Radiosynthesis of [11C]brofaromine, a potential tracer for imaging monoamine oxidase A.

    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

    pub_type： 杂志文章

    doi：10.1016/0969-8051(95)02051-9

    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

  • Pretargeted tumour imaging with streptavidin immunoconjugates of monoclonal antibody CC49 and 111In-DTPA-biocytin.

    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

    authors： Alvarez-Diez TM,Polihronis J,Reilly RM

    更新日期：1996-05-01 00:00:00

  • Fluoro analogs of WAY-100635 with varying pharmacokinetics properties.

    abstract：:Radiolabeled derivatives of WAY-100635 have been shown to be important for imaging in vivo because of their antagonist properties and their specificity for the 5-hydroxytryptamine(1A) (5-HT(1A)) receptor. Our goal is to prepare a series of radiofluorinated derivatives of WAY-100635 that, in the rat, range in pharmacok...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/s0969-8051(00)00111-6

    authors： Lang L,Jagoda E,Schmall B,Sassaman M,Ma Y,Eckelman WC

    更新日期：2000-07-01 00:00:00

  • Evaluation of [¹⁸F]PFH PET renography to predict future disease progression in a rat model of autosomal dominant polycystic kidney disease.

    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

    authors： Pathuri G,Hedrick AF,Awasthi V,Cowley BD Jr,Gali H

    更新日期：2016-01-01 00:00:00

  • An original radio-biomimetic approach to synthesize radiometabolites for PET imaging.

    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

    authors： Auvity S,Breuil L,Goislard M,Bottlaender M,Kuhnast B,Tournier N,Caillé F

    更新日期：2020-01-01 00:00:00

  • Preclinical and clinical evaluation of O-[11C]methyl-L-tyrosine for tumor imaging by positron emission tomography.

    abstract：:We performed preclinical and clinical studies of O-[11C]methyl-L-tyrosine, a potential tracer for imaging amino acid transport of tumors by positron emission tomography (PET). Examinations of the radiation-absorbed dose by O-[11C]methyl-L-tyrosine and the acute toxicity and mutagenicity of O-methyl-L-tyrosine showed s...

    journal_title：Nuclear medicine and biology

    pub_type： 临床试验,杂志文章

    doi：10.1016/j.nucmedbio.2004.11.005

    authors： Ishiwata K,Tsukada H,Kubota K,Nariai T,Harada N,Kawamura K,Kimura Y,Oda K,Iwata R,Ishii K

    更新日期：2005-04-01 00:00:00

  • Preparation of a multi-modal agent for sentinel lymph node mapping using Evans blue and 99mTc-labeled mannosylated human serum albumin conjugate.

    abstract：INTRODUCTION:The identification of sentinel lymph nodes (SLNs) is important in deciding the resection range during surgery. 99mTc-labeled mannosylated human serum albumin ([99mTc]Tc-MSA) is a radiopharmaceutical developed for SLN detection by targeting macrophages. Evans blue (EB) is a blue dye binding strongly to albu...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2020.02.002

    authors： Lee JY,Kim HY,Lee YS,Seo HY,Park JY,Jeong JM

    更新日期：2020-01-01 00:00:00

  • Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors.

    abstract：:The chemokine receptor CXCR4 is highly expressed in tumor cells and plays an important role in tumor metastasis. The aim of this study was to develop a radiopharmaceutical for the imaging of CXCR4-expressing tumors in vivo. Based on structure-activity relationships, we designed a 14-residue peptidic CXCR4 inhibitor, A...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2006.01.006

    authors： Hanaoka H,Mukai T,Tamamura H,Mori T,Ishino S,Ogawa K,Iida Y,Doi R,Fujii N,Saji H

    更新日期：2006-05-01 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

    doi：10.1016/s0969-8051(00)00159-1

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

    更新日期：2000-11-01 00:00:00

  • PET FDG studies in oncology.

    abstract：:Positron emission tomography (PET) studies of cancer with the glucose analog 2-[F-18]fluoro-2-deoxy-D-glucose (FDG) have emerged as both a useful research and clinical method for detecting (diagnosing), staging, and monitoring treatment responses in a variety of neoplasms, including tumors of the brain, head and neck,...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(94)90045-0

    authors： Hawkins RA,Hoh CK

    更新日期：1994-07-01 00:00:00

  • Chemical design of a radiolabeled gelatinase inhibitor peptide for the imaging of gelatinase activity in tumors.

    abstract：:Since elevated levels of gelatinases [matrix metalloproteinase (MMP)-2 and MMP-9] are associated with a poor prognosis in cancer patients, these enzymes are potential targets for tumor imaging. In the present study, a cyclic decapeptide, cCTTHWGFTLC (CTT), was selected as a mother compound because of its selective inh...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2007.04.002

    authors： Hanaoka H,Mukai T,Habashita S,Asano D,Ogawa K,Kuroda Y,Akizawa H,Iida Y,Endo K,Saga T,Saji H

    更新日期：2007-07-01 00:00:00

  • Application of image-derived and venous input functions in major depression using [carbonyl-(11)C]WAY-100635.

    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

    pub_type： 临床试验,杂志文章

    doi：10.1016/j.nucmedbio.2012.12.011

    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

  • Lipiodol solution of a lipophilic agent, (188)Re-TDD, for the treatment of liver cancer.

    abstract：:Radiolabeled lipiodol has been used for targeting liver cancer. We developed a lipiodol solution of (188)Re-TDD (2,2,9,9-tetramethyl-4,7-diaza-1,10-decanedithiol) and investigated its feasibility for the treatment of liver cancer. The lipiodol solution of (188)Re-TDD was well-retained in the lipiodol phase in vitro. A...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(00)00208-0

    authors： Jeong JM,Kim YJ,Lee YS,Ko JI,Son M,Lee DS,Chung JK,Park JH,Lee MC

    更新日期：2001-02-01 00:00:00

  • Evaluation of [11C]KB631 as a PET tracer for in vivo visualisation of HDAC6 in B16.F10 melanoma.

    abstract：INTRODUCTION:HDAC6, a structural and functional distinct member of the HDAC-family, shows great promise as a target to treat several cancers and neurodegenerative diseases. Several clinical trials are evaluating HDAC6 inhibitors in solid tumours and haematological malignancies, but so far no HDAC6 inhibitor has receive...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2019.05.004

    authors： Vermeulen K,Ahamed M,Luyten K,Bormans G

    更新日期：2019-01-01 00:00:00

  • Radiolabelling and positron emission tomography imaging of a high-affinity peptide binder to collagen type 1.

    abstract：INTRODUCTION:Pathological formation of fibrosis, is an important feature in many diseases. Fibrosis in liver and pancreas has been associated to metabolic disease including type 1 and 2 diabetes. The current methods for detecting and diagnosing fibrosis are either invasive, or their sensitivity to detect fibrosis in ea...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2020.11.006

    authors： Rosestedt M,Velikyan I,Rosenström U,Estrada S,Åberg O,Weis J,Westerlund C,Ingvast S,Korsgren O,Nordeman P,Eriksson O

    更新日期：2020-11-28 00:00:00

  • [11C]CURB: Evaluation of a novel radiotracer for imaging fatty acid amide hydrolase by positron emission tomography.

    abstract：INTRODUCTION:Fatty acid amide hydrolase (FAAH) is the enzyme responsible for metabolising the endogenous cannabinoid, anandamide, and thus represents an important target for molecular imaging. To date, no radiotracer has been shown to be useful for imaging of FAAH using either positron emission tomography (PET) or sing...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2010.08.001

    authors： Wilson AA,Garcia A,Parkes J,Houle S,Tong J,Vasdev N

    更新日期：2011-02-01 00:00:00

  • Does the anabolic metabolism of L-[2-18F]fluorophenylalanine and L-[2,6-3H]phenylalanine differ in the cerebrum and the cerebellum?

    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

    authors： Nakamichi H,Murakami M,Miura S,Kondoh Y,Mizusawa S,Ono Y

    更新日期：1994-10-01 00:00:00

  • Heterogeneity of plasma gonadotropins. Consequences on immunological properties of LH.

    abstract：:The pituitary gonadotropins FSH and LH are secreted into blood as dimeric glycoproteins which display a wide heterogeneity when submitted to technique of separation based on electric charge. That supports the assumption of a major role of the carbohydrates moieties as a source of heterogeneity. No clear difference how...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章,评审

    doi：10.1016/0969-8051(94)90058-2

    authors： Roger M,Lalhou N

    更新日期：1994-04-01 00:00:00

  • Synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine based on a cartridge purification method.

    abstract：INTRODUCTION:O-(2-[(18)F]fluoroethyl)-L-tyrosine (FET) is widely used as a positron emission tomography tracer for brain tumors. Usually, a high-performance liquid chromatography (HPLC) purification at the end of the two-step synthesis is applied. In this work, we report an automatic radiosynthesis of FET with a purifi...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2011.01.006

    authors： Mueller D,Klette I,Kalb F,Baum RP

    更新日期：2011-07-01 00:00:00

  • Scintimammography with Tc-99m MIBI in patients with suspicion of primary breast cancer.

    abstract：:The aim of the study was to evaluate the diagnostic accuracy of scintimammography with Tc-99m MIBI for the detection of breast cancer. Patients with a suspicious lesion detected by palpation or mammography were included in the study. Excisional biopsy was performed on all patients. Mammography was performed within 3 w...

    journal_title：Nuclear medicine and biology

    pub_type： 临床试验,杂志文章

    doi：10.1016/0969-8051(96)00084-4

    authors： Palmedo H,Schomburg A,Grünwald F,Mallmann P,Boldt I,Biersack HJ

    更新日期：1996-08-01 00:00:00

  • Impact of reversible trapping of tracer and the presence of blood metabolites on measurements of myocardial glucose utilization performed by PET and 18F-fluorodeoxyglucose using the Patlak method.

    abstract：:In this study we demonstrated that significant egress of FDG from myocardium occurs within the first hour after tracer injection leading to nonlinear Patlak plots. There are also significant amounts of acidic FDG metabolites present in the blood. However, the impact of these metabolites on the estimates of myocardial ...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2004.03.002

    authors： Herrero P,Dence CS,Sharp TL,Welch MJ,Gropler RJ

    更新日期：2004-10-01 00:00:00

  • Humanized versus murine anti-human epidermal growth factor receptor monoclonal antibodies for immunoscintigraphic studies.

    abstract：:The anti-human epidermal growth factor receptor (EGF-R) humanized antibody h-R3 (IgG(1)), which binds to an extracellular domain of EGF-R, was used to evaluate the biodistribution on nude mice xenografted with A431 epidermoid carcinoma cell line. Results are compared with its murine version ior egf/r3 monoclonal antib...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(99)00094-3

    authors： Morales AA,Ducongé J,Alvarez-Ruiz D,Becquer-Viart ML,Núñez-Gandolff G,Fernández E,Caballero-Torres I,Iznaga-Escobar N

    更新日期：2000-02-01 00:00:00

  • The chemical nature, purity and stability of 99mTc-N-(2,6-Diethyl-3-iodo-phenylcarbamoylmethyl)-iminodiacetic acid.

    abstract：:The chemical purity and stability of a radio pharmaceutical 99mTc-N-(2,6-diethyl-3-iodo-phenylcarbamoylmethyl)-iminodiacetic acid (IODIDA) has been studied using HPLC. The HPLC results indicate that IODIDA decomposed into at least three species after 99mTc labelling, and the amount of these varied with time. Mass spec...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/0969-8051(94)00120-9

    authors： Lundberg PS,Jacobsson L,Stenhagen G,Mårtensson J,Fjälling M

    更新日期：1995-05-01 00:00:00

  • Somatostatin receptor scintigraphy during treatment with lanreotide in patients with neuroendocrine tumors.

    abstract：:To investigate possible changes in somatostatin receptor expression during treatment with high dose lanreotide, eight patients with neuroendocrine tumors were investigated by [(111)In-DTPA-D-Phe1]-octreotide scintigraphy before and during treatment. The spleen-to-background ratio decreased in all patients, whereas tum...

    journal_title：Nuclear medicine and biology

    pub_type： 临床试验,杂志文章

    doi：10.1016/s0969-8051(99)00059-1

    authors： Janson ET,Kälkner KM,Eriksson B,Westlin JE,Oberg K

    更新日期：1999-11-01 00:00:00

  • Influence of the bifunctional chelate on the biological behavior of (99m)Tc-labeled chemotactic peptide conjugates.

    abstract：:Conjugates of For-MLFK and For-NleLFNleYK with S-benzyl mercaptoacetyl dipeptides containing, respectively, zero, one, and two carboxyl functions in their structures were prepared and labeled with (99m)Tc. In vitro binding studies using isolated human granulocytes indicated specific receptor binding of the radiolabele...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/s0969-8051(00)00168-2

    authors： Verbeke K,Snauwaert K,Cleynhens B,Scheers W,Verbruggen A

    更新日期：2000-11-01 00:00:00

  • Preparation and pharmacokinetics of 11C labeled stavudine (d4T).

    abstract：:Stavudine, a potent antiviral agent for treating human immunodeficiency virus (HIV) infections, was radiolabeled with (11)C by methylation of a specifically designed precursor, 5'-O-(2-tetrahydropyranyl)-5-bromo-2',3'-didehydro-3'-deoxythymidine, with (11)C H(3)I. The radiolabeled drug was isolated by reverse phase HP...

    journal_title：Nuclear medicine and biology

    pub_type： 杂志文章

    doi：10.1016/j.nucmedbio.2003.11.006

    authors： Livni E,Berker M,Hillier S,Waller SC,Ogan MD,Discordia RP,Rienhart JK,Rubin RH,Fischman AJ

    更新日期：2004-07-01 00:00:00

  • Methoxyphenylethynyl, methoxypyridylethynyl and phenylethynyl derivatives of pyridine: synthesis, radiolabeling and evaluation of new PET ligands for metabotropic glutamate subtype 5 receptors.

    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

    authors： Yu M,Tueckmantel W,Wang X,Zhu A,Kozikowski AP,Brownell AL

    更新日期：2005-08-01 00:00:00