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INSCAPE TERMINATED

Imaging Voltage Gated Sodium Channels Using Positron Emission Tomography

Total Cost €

0

EC-Contrib. €

0

Partnership

0

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 INSCAPE project word cloud

Explore the words cloud of the INSCAPE project. It provides you a very rough idea of what is the project "INSCAPE" about.

underlying    derivatives    nervous    revealing    emitting    therapies    fluorine    stability    ing    half    sodium    neurons    imaging    cns    vivo    pns    electrical    first    isoforms    neurodegenerative    probe    block    lifes    11    batrachotoxin    off    companies    scans    proteins    blockers    drugs    rodent    communication    rare    completely    tomography    investigation    transmembrane    tool    emission    truncated    potentially    channels    link    pain    severe    peripheral    small    human    valuable    thirdly    subsequently    11c    isotopes    neuronal    hot    navs    tested    pet    fluorescent    candidates    fast    nav    18    voltage    implicated    integral    pharmacokinetics    employed    function    nav1    pharmaceutical    positron    disclosed    drug    18f    benefits    therapy    assays    intensely    tr    central    global    signaling    labeled    secondly    synthesized    diseases    awaited    monitoring    pathogenesis    primary    btx    metabolic    carbon    gated    radioactive    society    purpose   

Project "INSCAPE" data sheet

The following table provides information about the project.

Coordinator
KLINIKUM DER UNIVERSITAET ZU KOELN 

Organization address
address: Kerpener Strasse 62
city: KOELN
postcode: 50937
website: www.uk-koeln.de

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country Germany [DE]
 Total cost 239˙860 €
 EC max contribution 239˙860 € (100%)
 Programme 1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
 Code Call H2020-MSCA-IF-2014
 Funding Scheme MSCA-IF-GF
 Starting year 2015
 Duration (year-month-day) from 2015-05-15   to  2018-05-14

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    KLINIKUM DER UNIVERSITAET ZU KOELN DE (KOELN) coordinator 239˙860.00
2    BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY US (STANFORD) partner 0.00

Map

 Project objective

Voltage gated sodium channels (NaVs) are the primary transmembrane proteins underlying fast electrical communication in neurons of the peripheral and central nervous system (PNS and CNS). Being such an integral part of neuronal signaling, they are implicated in a number of severe diseases that have a major impact on human society. However, drugs and established therapies targeting NaVs are rare due to common off-target effects. Therefore, new NaV-blockers will be developed and used for in vivo imaging using positron emission tomography (PET). For this purpose, novel derivatives of the recently disclosed truncated batrachotoxin (tr-BTX), which represent a completely new type of NaV-blockers, will be synthesized and their ability to block different NaV isoforms (NaV1.1 to 1.8) will be tested using fluorescent assays. The most promising candidates will then be labeled using different positron emitting isotopes such as carbon-11 (11C) and fluorine-18 (18F) exploiting different radioactive half-lifes and metabolic stability. The resulting “hot-tr-BTX” will be subsequently employed in small rodent PET-scans revealing their in vivo pharmacokinetics. This novel and unique tool will provide three major immediate benefits. First, hot-tr-BTX might deliver a general imaging probe for nervous activity in the PNS, and potentially the CNS, by monitoring NaV function in vivo. Secondly, this will allow the investigation of various pain conditions and neurodegenerative diseases and link their pathogenesis to NaV-function. Thirdly, the proposed research might deliver not only new NaV-blockers as potential drug candidates, but will also provide a valuable method facilitating the development of long awaited drugs targeting NaVs for pain therapy, a goal that is currently intensely investigated by numerous European and global pharmaceutical companies.

 Publications

year authors and title journal last update
List of publications.
2017 Matthias Schoenberger , Jacob Hooker , Martin Strebl , Al Schroeder , Timothy McKinsey , and Amrut Ambardekar
Imaging cardiac voltage gated sodium channels using the novel F-18 radiotracer radiocaine
published pages: , ISSN: , DOI:
2019-06-13
2017 Matthias Schoenberger, Frederick A. Schroeder, Michael S. Placzek, Randall L. Carter, Bruce R. Rosen, Jacob M. Hooker, Christin Y. Sander
In Vivo [ 18 F]GE-179 Brain Signal Does Not Show NMDA-Specific Modulation with Drug Challenges in Rodents and Nonhuman Primates
published pages: 298-305, ISSN: 1948-7193, DOI: 10.1021/acschemneuro.7b00327
ACS Chemical Neuroscience 9/2 2019-06-13

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