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  1. Article ; Online: A New Positron Emission Tomography Probe for Orexin Receptors Neuroimaging.

    Bai, Ping / Bai, Sha / Placzek, Michael S / Lu, Xiaoxia / Fiedler, Stephanie A / Ntaganda, Brenda / Wey, Hsiao-Ying / Wang, Changning

    Molecules (Basel, Switzerland)

    2020  Volume 25, Issue 5

    Abstract: The orexin receptor (OX) is critically involved in motivation and sleep-wake regulation and holds promising therapeutic potential in various mood disorders. To further investigate the role of orexin receptors (OXRs) in the living human brain and to ... ...

    Abstract The orexin receptor (OX) is critically involved in motivation and sleep-wake regulation and holds promising therapeutic potential in various mood disorders. To further investigate the role of orexin receptors (OXRs) in the living human brain and to evaluate the treatment potential of orexin-targeting therapeutics, we herein report a novel PET probe ([
    MeSH term(s) Brain/diagnostic imaging ; Brain/physiology ; Humans ; Neuroimaging ; Orexin Receptors/genetics ; Orexin Receptors/isolation & purification ; Positron-Emission Tomography ; Sleep/genetics ; Sleep/physiology
    Chemical Substances Orexin Receptors
    Language English
    Publishing date 2020-02-25
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules25051018
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  2. Article: Novel radioligands for imaging sigma-1 receptor in brain using positron emission tomography (PET).

    Lan, Yu / Bai, Ping / Chen, Zude / Neelamegam, Ramesh / Placzek, Michael S / Wang, Hao / Fiedler, Stephanie A / Yang, Jing / Yuan, Gengyang / Qu, Xiying / Schmidt, Hayden R / Song, Jinchun / Normandin, Marc D / Ran, Chongzhao / Wang, Changning

    Acta pharmaceutica Sinica. B

    2019  Volume 9, Issue 6, Page(s) 1204–1215

    Abstract: The sigma-1 receptor ( ...

    Abstract The sigma-1 receptor (
    Language English
    Publishing date 2019-07-11
    Publishing country Netherlands
    Document type Journal Article
    ISSN 2211-3835
    ISSN 2211-3835
    DOI 10.1016/j.apsb.2019.07.002
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Molecular imaging of Alzheimer's disease-related gamma-secretase in mice and nonhuman primates.

    Xu, Yulong / Wang, Changning / Wey, Hsiao-Ying / Liang, Yingxia / Chen, Zude / Choi, Se Hoon / Ran, Chongzhao / Rynearson, Kevin D / Bernales, Daniela R / Koegel, Robert E / Fiedler, Stephanie A / Striar, Robin / Wagner, Steven L / Tanzi, Rudolph E / Zhang, Can

    The Journal of experimental medicine

    2020  Volume 217, Issue 12

    Abstract: The pathogenesis of Alzheimer's disease (AD) is primarily driven by brain accumulation of the amyloid-β-42 (Aβ42) peptide generated from the amyloid-β precursor protein (APP) via cleavages by β- and γ-secretase. γ-Secretase is a prime drug target for AD; ...

    Abstract The pathogenesis of Alzheimer's disease (AD) is primarily driven by brain accumulation of the amyloid-β-42 (Aβ42) peptide generated from the amyloid-β precursor protein (APP) via cleavages by β- and γ-secretase. γ-Secretase is a prime drug target for AD; however, its brain regional expression and distribution remain largely unknown. Here, we are aimed at developing molecular imaging tools for visualizing γ-secretase. We used our recently developed γ-secretase modulators (GSMs) and synthesized our GSM-based imaging agent, [11C]SGSM-15606. We subsequently performed molecular imaging in rodents, including AD transgenic animals, and macaques, which revealed that our probe displayed good brain uptake and selectivity, stable metabolism, and appropriate kinetics and distribution for imaging γ-secretase in the brain. Interestingly, rodents and macaques shared certain brain areas with high γ-secretase expression, suggesting a functional conservation of γ-secretase. Collectively, we have provided the first molecular brain imaging of γ-secretase, which may not only accelerate our drug discovery for AD but also advance our understanding of AD.
    MeSH term(s) Alzheimer Disease/diagnostic imaging ; Alzheimer Disease/enzymology ; Amyloid Precursor Protein Secretases/metabolism ; Animals ; Brain/diagnostic imaging ; Brain/metabolism ; Brain/pathology ; Humans ; Macaca mulatta ; Magnetic Resonance Imaging ; Male ; Mice, Transgenic ; Molecular Imaging ; Positron Emission Tomography Computed Tomography ; Presenilin-1/metabolism
    Chemical Substances Presenilin-1 ; Amyloid Precursor Protein Secretases (EC 3.4.-)
    Language English
    Publishing date 2020-09-16
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 218343-2
    ISSN 1540-9538 ; 0022-1007
    ISSN (online) 1540-9538
    ISSN 0022-1007
    DOI 10.1084/jem.20182266
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Ua VI Zs.107: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MG 45: Show issues

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  4. Article ; Online: Imaging assisted evaluation of antitumor efficacy of a new histone deacetylase inhibitor in the castration-resistant prostate cancer.

    Chen, Zude / Wang, Xiashuang / Yang, Xiaoshuang / Xu, Yulong / Yang, Yu / Wang, Hao / Li, Tao / Bai, Ping / Yuan, Gengyang / Chen, Huabiao / Yang, Jing / Fiedler, Stephanie A / Striar, Robin / Bernales, Daniela R / Koegel, Robert E / Cao, Qi / Ran, Chongzhao / Xiang, Bo / Li, Hong /
    Wang, Changning

    European journal of nuclear medicine and molecular imaging

    2020  Volume 48, Issue 1, Page(s) 53–66

    Abstract: Purpose: Castration-resistant prostate cancer (CRPC) is the most common cause of death in men. The effectiveness of HDAC inhibitors has been demonstrated by preclinical models, but not in clinical studies, probably due to the ineffectively accumulation ... ...

    Abstract Purpose: Castration-resistant prostate cancer (CRPC) is the most common cause of death in men. The effectiveness of HDAC inhibitors has been demonstrated by preclinical models, but not in clinical studies, probably due to the ineffectively accumulation of HDACI in prostate cancer cells. The purpose of this work was to evaluate effects of a novel HDACI (CN133) on CRPC xenograft model and 22Rv1 cells, and develops methods, PET/CT imaging, to detect the therapeutic effects of CN133 on this cancer.
    Methods: We designed and performed study to compare the effects of CN133 with SAHA on the 22Rv1 xenograft model and 22Rv1 cells. Using PET/CT imaging with [
    Results: Our data showed that the CN133 treatment led to a 50% reduction of tumor volume compared to the placebo that was more efficacious than SAHA treatment in this preclinical model. [
    Conclusion: Taken together, these studies provide not only a novel epigenetic approach for prostate cancer therapy but also offering a potential tool, [
    MeSH term(s) Animals ; Cell Line, Tumor ; Cell Proliferation ; Histone Deacetylase Inhibitors/therapeutic use ; Humans ; Male ; Mice ; Positron Emission Tomography Computed Tomography ; Prostatic Neoplasms, Castration-Resistant/diagnostic imaging ; Prostatic Neoplasms, Castration-Resistant/drug therapy ; Xenograft Model Antitumor Assays
    Chemical Substances Histone Deacetylase Inhibitors
    Language English
    Publishing date 2020-06-26
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 8236-3
    ISSN 1619-7089 ; 0340-6997 ; 1619-7070
    ISSN (online) 1619-7089
    ISSN 0340-6997 ; 1619-7070
    DOI 10.1007/s00259-020-04896-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 1227: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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