Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter

Since the norepinephrine transporter (NET) is involved in a variety of diseases, the investigation of underlying dysregulation-mechanisms of the norepinephrine (NE) system is of major interest. Based on the previously described highly potent and selective NET ligand 1-(3-(methylamino)-1-phenylpropyl...

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Autores principales: Neudorfer, Catharina, Seddik, Amir, Shanab, Karem, Jurik, Andreas, Rami-Mark, Christina, Holzer, Wolfgang, Ecker, Gerhard, Mitterhauser, Markus, Wadsak, Wolfgang, Spreitzer, Helmut
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272146/
https://www.ncbi.nlm.nih.gov/pubmed/25608857
http://dx.doi.org/10.3390/molecules20011712
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author Neudorfer, Catharina
Seddik, Amir
Shanab, Karem
Jurik, Andreas
Rami-Mark, Christina
Holzer, Wolfgang
Ecker, Gerhard
Mitterhauser, Markus
Wadsak, Wolfgang
Spreitzer, Helmut
author_facet Neudorfer, Catharina
Seddik, Amir
Shanab, Karem
Jurik, Andreas
Rami-Mark, Christina
Holzer, Wolfgang
Ecker, Gerhard
Mitterhauser, Markus
Wadsak, Wolfgang
Spreitzer, Helmut
author_sort Neudorfer, Catharina
collection PubMed
description Since the norepinephrine transporter (NET) is involved in a variety of diseases, the investigation of underlying dysregulation-mechanisms of the norepinephrine (NE) system is of major interest. Based on the previously described highly potent and selective NET ligand 1-(3-(methylamino)-1-phenylpropyl)-3-phenyl-1,3-dihydro-2H-benzimidaz- ol-2-one (Me@APPI), this paper aims at the development of several fluorinated methylamine-based analogs of this compound. The newly synthesized compounds were computationally evaluated for their interactions with the monoamine transporters and represent reference compounds for PET-based investigation of the NET.
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spelling pubmed-62721462018-12-28 Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter Neudorfer, Catharina Seddik, Amir Shanab, Karem Jurik, Andreas Rami-Mark, Christina Holzer, Wolfgang Ecker, Gerhard Mitterhauser, Markus Wadsak, Wolfgang Spreitzer, Helmut Molecules Article Since the norepinephrine transporter (NET) is involved in a variety of diseases, the investigation of underlying dysregulation-mechanisms of the norepinephrine (NE) system is of major interest. Based on the previously described highly potent and selective NET ligand 1-(3-(methylamino)-1-phenylpropyl)-3-phenyl-1,3-dihydro-2H-benzimidaz- ol-2-one (Me@APPI), this paper aims at the development of several fluorinated methylamine-based analogs of this compound. The newly synthesized compounds were computationally evaluated for their interactions with the monoamine transporters and represent reference compounds for PET-based investigation of the NET. MDPI 2015-01-20 /pmc/articles/PMC6272146/ /pubmed/25608857 http://dx.doi.org/10.3390/molecules20011712 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Neudorfer, Catharina
Seddik, Amir
Shanab, Karem
Jurik, Andreas
Rami-Mark, Christina
Holzer, Wolfgang
Ecker, Gerhard
Mitterhauser, Markus
Wadsak, Wolfgang
Spreitzer, Helmut
Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title_full Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title_fullStr Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title_full_unstemmed Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title_short Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter
title_sort synthesis and in silico evaluation of novel compounds for pet-based investigations of the norepinephrine transporter
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272146/
https://www.ncbi.nlm.nih.gov/pubmed/25608857
http://dx.doi.org/10.3390/molecules20011712
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