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

Molecules

Catharina Neudorfer³  Amir Seddik¹  Karem Shanab³  Andreas Jurik¹  Christina Rami-Mark³  Wolfgang Holzer²  Gerhard Ecker¹  Markus Mitterhauser³  Wolfgang Wadsak³  Helmut Spreitzer² 

[1] Division of Drug Design and Medicinal Chemistry, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Althanstraße 14, 1090 Vienna, Austria; E-Mails:;Division of Drug Synthesis, Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Althanstraße 14, 1090 Vienna, Austria; E-Mail:;Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University of Vienna, Waehringer Guertel 18-20, 1090 Vienna, Austria; E-Mails:

关键词: NET;    ADHD;    cocaine dependence;    BAT;    PET;    FAPPI;   

DOI  :  10.3390/molecules20011712

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.