Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2019-12

AUTHORS

Kazunori Kawamura, Wakana Mori, Masayuki Fujinaga, Tomoteru Yamasaki, Yiding Zhang, Hidekatsu Wakizaka, Akiko Hatori, Lin Xie, Katsushi Kumata, Takayuki Ohkubo, Yusuke Kurihara, Masanao Ogawa, Nobuki Nengaki, Ming-Rong Zhang

ABSTRACT

Neuropeptide Y (NPY) has been implicated in a wide variety of physiological processes, including feeding, learning, memory, emotion, cardiovascular homeostasis, hormone secretion, and circadian rhythms. NPY Yl receptor (NPY Y1-R) is the most widely studied NPY receptor, and is involved in many of these processes. BMS-193885 (1) was previously developed as a potent and selective NPY Y1-R antagonist, which has good systemic bioavailability and brain penetration. To evaluate the characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its desmethyl analog ([11C]2) for potential use as two new positron emission tomography (PET) tracers. [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was synthesized from [11C]phosgene using its aniline and amine derivatives. The mean ± S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the end of radionuclide production were 23 ± 3.2% (n = 6) and 24 ± 1.5% (n = 4), respectively. In biodistribution on mice, radioactivity levels for both tracers were relatively high in the kidney, small intestine, and liver at 60 min post-injection. The radioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection with [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of [11C]1 in the brain of mice were significantly increased by pretreatment with the P-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg). In metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly metabolized within 30 min post-injection, and [11C]1 was mainly metabolized into unlabeled 2 and radiolabeled components. [11C]1 and [11C]2 were successfully synthesized with sufficient amount of radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl analog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1. More... »

PAGES

4

Identifiers

URI

http://scigraph.springernature.com/pub.10.1186/s41181-019-0056-5

DOI

http://dx.doi.org/10.1186/s41181-019-0056-5

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1112217073


Indexing Status Check whether this publication has been indexed by Scopus and Web Of Science using the SN Indexing Status Tool
Incoming Citations Browse incoming citations for this publication using opencitations.net

JSON-LD is the canonical representation for SciGraph data.

TIP: You can open this SciGraph record using an external JSON-LD service: JSON-LD Playground Google SDTT

[
  {
    "@context": "https://springernature.github.io/scigraph/jsonld/sgcontext.json", 
    "about": [
      {
        "id": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/1109", 
        "inDefinedTermSet": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/", 
        "name": "Neurosciences", 
        "type": "DefinedTerm"
      }, 
      {
        "id": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/11", 
        "inDefinedTermSet": "http://purl.org/au-research/vocabulary/anzsrc-for/2008/", 
        "name": "Medical and Health Sciences", 
        "type": "DefinedTerm"
      }
    ], 
    "author": [
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Kawamura", 
        "givenName": "Kazunori", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Mori", 
        "givenName": "Wakana", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Fujinaga", 
        "givenName": "Masayuki", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Yamasaki", 
        "givenName": "Tomoteru", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Zhang", 
        "givenName": "Yiding", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Medical Physics, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Wakizaka", 
        "givenName": "Hidekatsu", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Hatori", 
        "givenName": "Akiko", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Xie", 
        "givenName": "Lin", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Kumata", 
        "givenName": "Katsushi", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Sumitomo Heavy Industries (Japan)", 
          "id": "https://www.grid.ac/institutes/grid.471313.3", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan", 
            "SHI Accelerator Service Ltd, 141-0032, Tokyo, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Ohkubo", 
        "givenName": "Takayuki", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Sumitomo Heavy Industries (Japan)", 
          "id": "https://www.grid.ac/institutes/grid.471313.3", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan", 
            "SHI Accelerator Service Ltd, 141-0032, Tokyo, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Kurihara", 
        "givenName": "Yusuke", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Sumitomo Heavy Industries (Japan)", 
          "id": "https://www.grid.ac/institutes/grid.471313.3", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan", 
            "SHI Accelerator Service Ltd, 141-0032, Tokyo, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Ogawa", 
        "givenName": "Masanao", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "Sumitomo Heavy Industries (Japan)", 
          "id": "https://www.grid.ac/institutes/grid.471313.3", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan", 
            "SHI Accelerator Service Ltd, 141-0032, Tokyo, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Nengaki", 
        "givenName": "Nobuki", 
        "type": "Person"
      }, 
      {
        "affiliation": {
          "alternateName": "National Institute of Radiological Sciences", 
          "id": "https://www.grid.ac/institutes/grid.419638.1", 
          "name": [
            "Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan"
          ], 
          "type": "Organization"
        }, 
        "familyName": "Zhang", 
        "givenName": "Ming-Rong", 
        "type": "Person"
      }
    ], 
    "citation": [
      {
        "id": "https://doi.org/10.1073/pnas.89.13.5794", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1001513756"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1074/jbc.270.50.30102", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1003861514"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1073/pnas.82.11.3940", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1004105043"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1002/cne.10303", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1004882325"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/s0969-8051(00)00125-6", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1004959548"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.bmcl.2009.12.068", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1007404304"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1097/00001756-199604100-00020", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1017245412"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1097/00001756-199604100-00020", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1017245412"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1097/00001756-199604100-00020", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1017245412"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.npep.2004.05.005", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1018482796"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1046/j.1460-9568.1999.00553.x", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1018657510"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.bmcl.2009.07.030", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1023715800"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.peptides.2005.04.018", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1024088198"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.peptides.2005.04.018", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1024088198"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.ejphar.2008.06.032", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1024802660"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.nucmedbio.2009.08.008", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1026828587"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.nucmedbio.2009.07.004", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1027223360"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1139/y06-106", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1027796728"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.nucmedbio.2004.12.005", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1028242870"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1073/pnas.79.8.2514", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1034548222"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/s0960-894x(01)00761-2", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1034620950"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.chroma.2007.10.084", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1036416775"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.nucmedbio.2013.03.004", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1038235999"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/s0969-8043(00)00392-4", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1039700798"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/0196-9781(89)90176-9", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1043709799"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1111/j.1748-1716.1982.tb07171.x", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1047767221"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "sg:pub.10.1038/296659a0", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1052097635", 
          "https://doi.org/10.1038/296659a0"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1016/j.neuroimage.2010.11.014", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1052828907"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/acs.molpharmaceut.6b00464", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1055120409"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/bc015514h", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1055153250"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/bc015514h", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1055153250"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/bc7004297", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1055155416"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/bc7004297", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1055155416"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1210/endo-115-1-427", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1064258144"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1289/ehp.94102s1175", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1064745483"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1021/acsmedchemlett.6b00467", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1083882525"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "sg:pub.10.1038/s41586-018-0046-x", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1103428409", 
          "https://doi.org/10.1038/s41586-018-0046-x"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "sg:pub.10.1038/s41586-018-0046-x", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1103428409", 
          "https://doi.org/10.1038/s41586-018-0046-x"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1124/dmd.118.082958", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1105981115"
        ], 
        "type": "CreativeWork"
      }, 
      {
        "id": "https://doi.org/10.1124/dmd.118.082958", 
        "sameAs": [
          "https://app.dimensions.ai/details/publication/pub.1105981115"
        ], 
        "type": "CreativeWork"
      }
    ], 
    "datePublished": "2019-12", 
    "datePublishedReg": "2019-12-01", 
    "description": "Neuropeptide Y (NPY) has been implicated in a wide variety of physiological processes, including feeding, learning, memory, emotion, cardiovascular homeostasis, hormone secretion, and circadian rhythms. NPY Yl receptor (NPY Y1-R) is the most widely studied NPY receptor, and is involved in many of these processes. BMS-193885 (1) was previously developed as a potent and selective NPY Y1-R antagonist, which has good systemic bioavailability and brain penetration. To evaluate the characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its desmethyl analog ([11C]2) for potential use as two new positron emission tomography (PET) tracers. [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was synthesized from [11C]phosgene using its aniline and amine derivatives. The mean \u00b1 S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the end of radionuclide production were 23 \u00b1 3.2% (n = 6) and 24 \u00b1 1.5% (n = 4), respectively. In biodistribution on mice, radioactivity levels for both tracers were relatively high in the kidney, small intestine, and liver at 60 min post-injection. The radioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection with [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of [11C]1 in the brain of mice were significantly increased by pretreatment with the P-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg). In metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly metabolized within 30 min post-injection, and [11C]1 was mainly metabolized into unlabeled 2 and radiolabeled components. [11C]1 and [11C]2 were successfully synthesized with sufficient amount of radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl analog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1.", 
    "genre": "research_article", 
    "id": "sg:pub.10.1186/s41181-019-0056-5", 
    "inLanguage": [
      "en"
    ], 
    "isAccessibleForFree": false, 
    "isFundedItemOf": [
      {
        "id": "sg:grant.6143999", 
        "type": "MonetaryGrant"
      }
    ], 
    "isPartOf": [
      {
        "id": "sg:journal.1157056", 
        "issn": [
          "2365-421X"
        ], 
        "name": "EJNMMI Radiopharmacy and Chemistry", 
        "type": "Periodical"
      }, 
      {
        "issueNumber": "1", 
        "type": "PublicationIssue"
      }, 
      {
        "type": "PublicationVolume", 
        "volumeNumber": "4"
      }
    ], 
    "name": "Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors", 
    "pagination": "4", 
    "productId": [
      {
        "name": "doi", 
        "type": "PropertyValue", 
        "value": [
          "10.1186/s41181-019-0056-5"
        ]
      }, 
      {
        "name": "readcube_id", 
        "type": "PropertyValue", 
        "value": [
          "872f1202a4a7acac3795033637fab4553f1fa4cf6e128f1e9f43de99ff3d2c3b"
        ]
      }, 
      {
        "name": "dimensions_id", 
        "type": "PropertyValue", 
        "value": [
          "pub.1112217073"
        ]
      }
    ], 
    "sameAs": [
      "https://doi.org/10.1186/s41181-019-0056-5", 
      "https://app.dimensions.ai/details/publication/pub.1112217073"
    ], 
    "sdDataset": "articles", 
    "sdDatePublished": "2019-04-15T09:11", 
    "sdLicense": "https://scigraph.springernature.com/explorer/license/", 
    "sdPublisher": {
      "name": "Springer Nature - SN SciGraph project", 
      "type": "Organization"
    }, 
    "sdSource": "s3://com-uberresearch-data-dimensions-target-20181106-alternative/cleanup/v134/2549eaecd7973599484d7c17b260dba0a4ecb94b/merge/v9/a6c9fde33151104705d4d7ff012ea9563521a3ce/jats-lookup/v90/0000000376_0000000376/records_56158_00000006.jsonl", 
    "type": "ScholarlyArticle", 
    "url": "https://link.springer.com/10.1186%2Fs41181-019-0056-5"
  }
]
 

Download the RDF metadata as:  json-ld nt turtle xml License info

HOW TO GET THIS DATA PROGRAMMATICALLY:

JSON-LD is a popular format for linked data which is fully compatible with JSON.

curl -H 'Accept: application/ld+json' 'https://scigraph.springernature.com/pub.10.1186/s41181-019-0056-5'

N-Triples is a line-based linked data format ideal for batch operations.

curl -H 'Accept: application/n-triples' 'https://scigraph.springernature.com/pub.10.1186/s41181-019-0056-5'

Turtle is a human-readable linked data format.

curl -H 'Accept: text/turtle' 'https://scigraph.springernature.com/pub.10.1186/s41181-019-0056-5'

RDF/XML is a standard XML format for linked data.

curl -H 'Accept: application/rdf+xml' 'https://scigraph.springernature.com/pub.10.1186/s41181-019-0056-5'


 

This table displays all metadata directly associated to this object as RDF triples.

245 TRIPLES      21 PREDICATES      60 URIs      19 LITERALS      7 BLANK NODES

Subject Predicate Object
1 sg:pub.10.1186/s41181-019-0056-5 schema:about anzsrc-for:11
2 anzsrc-for:1109
3 schema:author N43c7d537a63c422487ae2165b6285fdd
4 schema:citation sg:pub.10.1038/296659a0
5 sg:pub.10.1038/s41586-018-0046-x
6 https://doi.org/10.1002/cne.10303
7 https://doi.org/10.1016/0196-9781(89)90176-9
8 https://doi.org/10.1016/j.bmcl.2009.07.030
9 https://doi.org/10.1016/j.bmcl.2009.12.068
10 https://doi.org/10.1016/j.chroma.2007.10.084
11 https://doi.org/10.1016/j.ejphar.2008.06.032
12 https://doi.org/10.1016/j.neuroimage.2010.11.014
13 https://doi.org/10.1016/j.npep.2004.05.005
14 https://doi.org/10.1016/j.nucmedbio.2004.12.005
15 https://doi.org/10.1016/j.nucmedbio.2009.07.004
16 https://doi.org/10.1016/j.nucmedbio.2009.08.008
17 https://doi.org/10.1016/j.nucmedbio.2013.03.004
18 https://doi.org/10.1016/j.peptides.2005.04.018
19 https://doi.org/10.1016/s0960-894x(01)00761-2
20 https://doi.org/10.1016/s0969-8043(00)00392-4
21 https://doi.org/10.1016/s0969-8051(00)00125-6
22 https://doi.org/10.1021/acs.molpharmaceut.6b00464
23 https://doi.org/10.1021/acsmedchemlett.6b00467
24 https://doi.org/10.1021/bc015514h
25 https://doi.org/10.1021/bc7004297
26 https://doi.org/10.1046/j.1460-9568.1999.00553.x
27 https://doi.org/10.1073/pnas.79.8.2514
28 https://doi.org/10.1073/pnas.82.11.3940
29 https://doi.org/10.1073/pnas.89.13.5794
30 https://doi.org/10.1074/jbc.270.50.30102
31 https://doi.org/10.1097/00001756-199604100-00020
32 https://doi.org/10.1111/j.1748-1716.1982.tb07171.x
33 https://doi.org/10.1124/dmd.118.082958
34 https://doi.org/10.1139/y06-106
35 https://doi.org/10.1210/endo-115-1-427
36 https://doi.org/10.1289/ehp.94102s1175
37 schema:datePublished 2019-12
38 schema:datePublishedReg 2019-12-01
39 schema:description Neuropeptide Y (NPY) has been implicated in a wide variety of physiological processes, including feeding, learning, memory, emotion, cardiovascular homeostasis, hormone secretion, and circadian rhythms. NPY Yl receptor (NPY Y1-R) is the most widely studied NPY receptor, and is involved in many of these processes. BMS-193885 (1) was previously developed as a potent and selective NPY Y1-R antagonist, which has good systemic bioavailability and brain penetration. To evaluate the characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its desmethyl analog ([11C]2) for potential use as two new positron emission tomography (PET) tracers. [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was synthesized from [11C]phosgene using its aniline and amine derivatives. The mean ± S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the end of radionuclide production were 23 ± 3.2% (n = 6) and 24 ± 1.5% (n = 4), respectively. In biodistribution on mice, radioactivity levels for both tracers were relatively high in the kidney, small intestine, and liver at 60 min post-injection. The radioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection with [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of [11C]1 in the brain of mice were significantly increased by pretreatment with the P-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg). In metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly metabolized within 30 min post-injection, and [11C]1 was mainly metabolized into unlabeled 2 and radiolabeled components. [11C]1 and [11C]2 were successfully synthesized with sufficient amount of radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl analog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1.
40 schema:genre research_article
41 schema:inLanguage en
42 schema:isAccessibleForFree false
43 schema:isPartOf N577bfea8acfb4899960a4f17a6d0e76b
44 N7550c35a6d6046cebaa53c3d283375ec
45 sg:journal.1157056
46 schema:name Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors
47 schema:pagination 4
48 schema:productId N0ee5843efdba4edabf7369adc5a20a0d
49 N4b1372669cde4b6f8fe980acd057123d
50 Nd333cc3840f94700ac82bdfce0f7ca30
51 schema:sameAs https://app.dimensions.ai/details/publication/pub.1112217073
52 https://doi.org/10.1186/s41181-019-0056-5
53 schema:sdDatePublished 2019-04-15T09:11
54 schema:sdLicense https://scigraph.springernature.com/explorer/license/
55 schema:sdPublisher N58e505b8a7ee431bb1a64939f2b78b89
56 schema:url https://link.springer.com/10.1186%2Fs41181-019-0056-5
57 sgo:license sg:explorer/license/
58 sgo:sdDataset articles
59 rdf:type schema:ScholarlyArticle
60 N0770e5615aad494b8663ef8e490d250c schema:affiliation https://www.grid.ac/institutes/grid.471313.3
61 schema:familyName Nengaki
62 schema:givenName Nobuki
63 rdf:type schema:Person
64 N0ee22206e5b54f24a2db144d9a685eb4 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
65 schema:familyName Yamasaki
66 schema:givenName Tomoteru
67 rdf:type schema:Person
68 N0ee5843efdba4edabf7369adc5a20a0d schema:name readcube_id
69 schema:value 872f1202a4a7acac3795033637fab4553f1fa4cf6e128f1e9f43de99ff3d2c3b
70 rdf:type schema:PropertyValue
71 N22737103898c4b7da1a5c94eb486c06e rdf:first N0ee22206e5b54f24a2db144d9a685eb4
72 rdf:rest Nb5de100eda6c439c8e415ce96baf2e46
73 N3455fa07997043159fa434b881859ed7 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
74 schema:familyName Kumata
75 schema:givenName Katsushi
76 rdf:type schema:Person
77 N3d26abd08e7d403682b2c5c43ad5536e schema:affiliation https://www.grid.ac/institutes/grid.471313.3
78 schema:familyName Ohkubo
79 schema:givenName Takayuki
80 rdf:type schema:Person
81 N3d4dfae2cbe94694b871316f9801668a rdf:first Na5ae38d18ad34db1b64f93ddc7cc1a44
82 rdf:rest N8a9885f644a745a8a426eaf328a0f315
83 N43c7d537a63c422487ae2165b6285fdd rdf:first Nee3eb9c8f5f34aeca85822bc58bed5e2
84 rdf:rest N98843191e92745c1b0eddd48357895fc
85 N489b7cf4e9df48a3b52bb9b7188cf9d2 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
86 schema:familyName Xie
87 schema:givenName Lin
88 rdf:type schema:Person
89 N4b1372669cde4b6f8fe980acd057123d schema:name doi
90 schema:value 10.1186/s41181-019-0056-5
91 rdf:type schema:PropertyValue
92 N577bfea8acfb4899960a4f17a6d0e76b schema:issueNumber 1
93 rdf:type schema:PublicationIssue
94 N58e505b8a7ee431bb1a64939f2b78b89 schema:name Springer Nature - SN SciGraph project
95 rdf:type schema:Organization
96 N6d8d8b31150c4cf3ac78cedeaf02cd1d rdf:first N8da614889baf4d5e85aeefdf768732da
97 rdf:rest rdf:nil
98 N7550c35a6d6046cebaa53c3d283375ec schema:volumeNumber 4
99 rdf:type schema:PublicationVolume
100 N7bec11adf8f246e482e375928e4f1dd3 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
101 schema:familyName Wakizaka
102 schema:givenName Hidekatsu
103 rdf:type schema:Person
104 N82a139c7b480421d9aec95bf724bd2fd rdf:first N3455fa07997043159fa434b881859ed7
105 rdf:rest Nbee0730e9c794701920c40ff4da1943e
106 N8a9885f644a745a8a426eaf328a0f315 rdf:first N0770e5615aad494b8663ef8e490d250c
107 rdf:rest N6d8d8b31150c4cf3ac78cedeaf02cd1d
108 N8da614889baf4d5e85aeefdf768732da schema:affiliation https://www.grid.ac/institutes/grid.419638.1
109 schema:familyName Zhang
110 schema:givenName Ming-Rong
111 rdf:type schema:Person
112 N98843191e92745c1b0eddd48357895fc rdf:first Nc6ede4eca2564fc08f2e3272a3a306aa
113 rdf:rest Naa26f537c9b8490ba5abdd8f680f3fc4
114 N9925134a9420480eb46ec0064b192257 schema:affiliation https://www.grid.ac/institutes/grid.471313.3
115 schema:familyName Kurihara
116 schema:givenName Yusuke
117 rdf:type schema:Person
118 Na5ae38d18ad34db1b64f93ddc7cc1a44 schema:affiliation https://www.grid.ac/institutes/grid.471313.3
119 schema:familyName Ogawa
120 schema:givenName Masanao
121 rdf:type schema:Person
122 Naa26f537c9b8490ba5abdd8f680f3fc4 rdf:first Nc9b68ec203cc4be9a8433395790100c8
123 rdf:rest N22737103898c4b7da1a5c94eb486c06e
124 Naf39094c9e1a424990617f4a455ebacd rdf:first N9925134a9420480eb46ec0064b192257
125 rdf:rest N3d4dfae2cbe94694b871316f9801668a
126 Nb5de100eda6c439c8e415ce96baf2e46 rdf:first Nd5fb91ab1699437881679153e9db429c
127 rdf:rest Ne3eabfad64db43f2a0da04c9b98e3714
128 Nbee0730e9c794701920c40ff4da1943e rdf:first N3d26abd08e7d403682b2c5c43ad5536e
129 rdf:rest Naf39094c9e1a424990617f4a455ebacd
130 Nc6ede4eca2564fc08f2e3272a3a306aa schema:affiliation https://www.grid.ac/institutes/grid.419638.1
131 schema:familyName Mori
132 schema:givenName Wakana
133 rdf:type schema:Person
134 Nc9b68ec203cc4be9a8433395790100c8 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
135 schema:familyName Fujinaga
136 schema:givenName Masayuki
137 rdf:type schema:Person
138 Nd333cc3840f94700ac82bdfce0f7ca30 schema:name dimensions_id
139 schema:value pub.1112217073
140 rdf:type schema:PropertyValue
141 Nd5fb91ab1699437881679153e9db429c schema:affiliation https://www.grid.ac/institutes/grid.419638.1
142 schema:familyName Zhang
143 schema:givenName Yiding
144 rdf:type schema:Person
145 Ndb623aafb33340f688136e9718d5b78d rdf:first N489b7cf4e9df48a3b52bb9b7188cf9d2
146 rdf:rest N82a139c7b480421d9aec95bf724bd2fd
147 Ndbd83343454d4d61b202f35081469a5e schema:affiliation https://www.grid.ac/institutes/grid.419638.1
148 schema:familyName Hatori
149 schema:givenName Akiko
150 rdf:type schema:Person
151 Ne3e0783fcbe84077820b1a0db7fa57d5 rdf:first Ndbd83343454d4d61b202f35081469a5e
152 rdf:rest Ndb623aafb33340f688136e9718d5b78d
153 Ne3eabfad64db43f2a0da04c9b98e3714 rdf:first N7bec11adf8f246e482e375928e4f1dd3
154 rdf:rest Ne3e0783fcbe84077820b1a0db7fa57d5
155 Nee3eb9c8f5f34aeca85822bc58bed5e2 schema:affiliation https://www.grid.ac/institutes/grid.419638.1
156 schema:familyName Kawamura
157 schema:givenName Kazunori
158 rdf:type schema:Person
159 anzsrc-for:11 schema:inDefinedTermSet anzsrc-for:
160 schema:name Medical and Health Sciences
161 rdf:type schema:DefinedTerm
162 anzsrc-for:1109 schema:inDefinedTermSet anzsrc-for:
163 schema:name Neurosciences
164 rdf:type schema:DefinedTerm
165 sg:grant.6143999 http://pending.schema.org/fundedItem sg:pub.10.1186/s41181-019-0056-5
166 rdf:type schema:MonetaryGrant
167 sg:journal.1157056 schema:issn 2365-421X
168 schema:name EJNMMI Radiopharmacy and Chemistry
169 rdf:type schema:Periodical
170 sg:pub.10.1038/296659a0 schema:sameAs https://app.dimensions.ai/details/publication/pub.1052097635
171 https://doi.org/10.1038/296659a0
172 rdf:type schema:CreativeWork
173 sg:pub.10.1038/s41586-018-0046-x schema:sameAs https://app.dimensions.ai/details/publication/pub.1103428409
174 https://doi.org/10.1038/s41586-018-0046-x
175 rdf:type schema:CreativeWork
176 https://doi.org/10.1002/cne.10303 schema:sameAs https://app.dimensions.ai/details/publication/pub.1004882325
177 rdf:type schema:CreativeWork
178 https://doi.org/10.1016/0196-9781(89)90176-9 schema:sameAs https://app.dimensions.ai/details/publication/pub.1043709799
179 rdf:type schema:CreativeWork
180 https://doi.org/10.1016/j.bmcl.2009.07.030 schema:sameAs https://app.dimensions.ai/details/publication/pub.1023715800
181 rdf:type schema:CreativeWork
182 https://doi.org/10.1016/j.bmcl.2009.12.068 schema:sameAs https://app.dimensions.ai/details/publication/pub.1007404304
183 rdf:type schema:CreativeWork
184 https://doi.org/10.1016/j.chroma.2007.10.084 schema:sameAs https://app.dimensions.ai/details/publication/pub.1036416775
185 rdf:type schema:CreativeWork
186 https://doi.org/10.1016/j.ejphar.2008.06.032 schema:sameAs https://app.dimensions.ai/details/publication/pub.1024802660
187 rdf:type schema:CreativeWork
188 https://doi.org/10.1016/j.neuroimage.2010.11.014 schema:sameAs https://app.dimensions.ai/details/publication/pub.1052828907
189 rdf:type schema:CreativeWork
190 https://doi.org/10.1016/j.npep.2004.05.005 schema:sameAs https://app.dimensions.ai/details/publication/pub.1018482796
191 rdf:type schema:CreativeWork
192 https://doi.org/10.1016/j.nucmedbio.2004.12.005 schema:sameAs https://app.dimensions.ai/details/publication/pub.1028242870
193 rdf:type schema:CreativeWork
194 https://doi.org/10.1016/j.nucmedbio.2009.07.004 schema:sameAs https://app.dimensions.ai/details/publication/pub.1027223360
195 rdf:type schema:CreativeWork
196 https://doi.org/10.1016/j.nucmedbio.2009.08.008 schema:sameAs https://app.dimensions.ai/details/publication/pub.1026828587
197 rdf:type schema:CreativeWork
198 https://doi.org/10.1016/j.nucmedbio.2013.03.004 schema:sameAs https://app.dimensions.ai/details/publication/pub.1038235999
199 rdf:type schema:CreativeWork
200 https://doi.org/10.1016/j.peptides.2005.04.018 schema:sameAs https://app.dimensions.ai/details/publication/pub.1024088198
201 rdf:type schema:CreativeWork
202 https://doi.org/10.1016/s0960-894x(01)00761-2 schema:sameAs https://app.dimensions.ai/details/publication/pub.1034620950
203 rdf:type schema:CreativeWork
204 https://doi.org/10.1016/s0969-8043(00)00392-4 schema:sameAs https://app.dimensions.ai/details/publication/pub.1039700798
205 rdf:type schema:CreativeWork
206 https://doi.org/10.1016/s0969-8051(00)00125-6 schema:sameAs https://app.dimensions.ai/details/publication/pub.1004959548
207 rdf:type schema:CreativeWork
208 https://doi.org/10.1021/acs.molpharmaceut.6b00464 schema:sameAs https://app.dimensions.ai/details/publication/pub.1055120409
209 rdf:type schema:CreativeWork
210 https://doi.org/10.1021/acsmedchemlett.6b00467 schema:sameAs https://app.dimensions.ai/details/publication/pub.1083882525
211 rdf:type schema:CreativeWork
212 https://doi.org/10.1021/bc015514h schema:sameAs https://app.dimensions.ai/details/publication/pub.1055153250
213 rdf:type schema:CreativeWork
214 https://doi.org/10.1021/bc7004297 schema:sameAs https://app.dimensions.ai/details/publication/pub.1055155416
215 rdf:type schema:CreativeWork
216 https://doi.org/10.1046/j.1460-9568.1999.00553.x schema:sameAs https://app.dimensions.ai/details/publication/pub.1018657510
217 rdf:type schema:CreativeWork
218 https://doi.org/10.1073/pnas.79.8.2514 schema:sameAs https://app.dimensions.ai/details/publication/pub.1034548222
219 rdf:type schema:CreativeWork
220 https://doi.org/10.1073/pnas.82.11.3940 schema:sameAs https://app.dimensions.ai/details/publication/pub.1004105043
221 rdf:type schema:CreativeWork
222 https://doi.org/10.1073/pnas.89.13.5794 schema:sameAs https://app.dimensions.ai/details/publication/pub.1001513756
223 rdf:type schema:CreativeWork
224 https://doi.org/10.1074/jbc.270.50.30102 schema:sameAs https://app.dimensions.ai/details/publication/pub.1003861514
225 rdf:type schema:CreativeWork
226 https://doi.org/10.1097/00001756-199604100-00020 schema:sameAs https://app.dimensions.ai/details/publication/pub.1017245412
227 rdf:type schema:CreativeWork
228 https://doi.org/10.1111/j.1748-1716.1982.tb07171.x schema:sameAs https://app.dimensions.ai/details/publication/pub.1047767221
229 rdf:type schema:CreativeWork
230 https://doi.org/10.1124/dmd.118.082958 schema:sameAs https://app.dimensions.ai/details/publication/pub.1105981115
231 rdf:type schema:CreativeWork
232 https://doi.org/10.1139/y06-106 schema:sameAs https://app.dimensions.ai/details/publication/pub.1027796728
233 rdf:type schema:CreativeWork
234 https://doi.org/10.1210/endo-115-1-427 schema:sameAs https://app.dimensions.ai/details/publication/pub.1064258144
235 rdf:type schema:CreativeWork
236 https://doi.org/10.1289/ehp.94102s1175 schema:sameAs https://app.dimensions.ai/details/publication/pub.1064745483
237 rdf:type schema:CreativeWork
238 https://www.grid.ac/institutes/grid.419638.1 schema:alternateName National Institute of Radiological Sciences
239 schema:name Department of Medical Physics, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 263-8555, Chiba, Japan
240 Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan
241 rdf:type schema:Organization
242 https://www.grid.ac/institutes/grid.471313.3 schema:alternateName Sumitomo Heavy Industries (Japan)
243 schema:name Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, 4-9-1 Anagawa, Inage-ku, 263-8555, Chiba, Japan
244 SHI Accelerator Service Ltd, 141-0032, Tokyo, Japan
245 rdf:type schema:Organization
 




Preview window. Press ESC to close (or click here)


...