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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.

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

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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