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Molecules 2015, 20(1), 1712-1730; doi:10.3390/molecules20011712

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

1
Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, 1090 Vienna, Austria
2
Division of Drug Synthesis, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Althanstraße 14, 1090 Vienna, Austria
3
Division of Drug Design and Medicinal Chemistry, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Althanstraße 14, 1090 Vienna, Austria
*
Authors to whom correspondence should be addressed.
Academic Editor: Svend Borup Jensen
Received: 20 November 2014 / Revised: 7 January 2015 / Accepted: 14 January 2015 / Published: 20 January 2015
(This article belongs to the Special Issue Preparation of Radiopharmaceuticals and Their Use in Drug Development)
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Abstract

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. View Full-Text
Keywords: NET; ADHD; cocaine dependence; BAT; PET; FAPPI NET; ADHD; cocaine dependence; BAT; PET; FAPPI
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Neudorfer, C.; Seddik, A.; Shanab, K.; Jurik, A.; Rami-Mark, C.; Holzer, W.; Ecker, G.; Mitterhauser, M.; Wadsak, W.; Spreitzer, H. Synthesis and in Silico Evaluation of Novel Compounds for PET-Based Investigations of the Norepinephrine Transporter. Molecules 2015, 20, 1712-1730.

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