Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-11C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ1-Receptor–Targeted PET Imaging

Achi Haider; Adrienne Müller Herde; Stefanie D. Krämer; Jasmine Varisco; Claudia Keller; Katrin Frauenknecht; Yves P. Auberson; Louisa Temme; Dina Robaa; Wolfgang Sippl; Roger Schibli; Bernhard Wünsch; Linjing Mu; Simon M. Ametamey

doi:10.2967/jnumed.118.221051

Research ArticleRadiochemistry

Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-¹¹C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ₁-Receptor–Targeted PET Imaging

Achi Haider, Adrienne Müller Herde, Stefanie D. Krämer, Jasmine Varisco, Claudia Keller, Katrin Frauenknecht, Yves P. Auberson, Louisa Temme, Dina Robaa, Wolfgang Sippl, Roger Schibli, Bernhard Wünsch, Linjing Mu and Simon M. Ametamey

Journal of Nuclear Medicine August 2019, 60 (8) 1167-1173; DOI: https://doi.org/10.2967/jnumed.118.221051

Achi Haider

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Adrienne Müller Herde

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Stefanie D. Krämer

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Jasmine Varisco

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Claudia Keller

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Katrin Frauenknecht

2Institute of Neuropathology, University of Zurich/University Hospital Zurich, Zurich, Switzerland

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Yves P. Auberson

3Novartis Institutes for BioMedical Research, Basel, Switzerland

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Louisa Temme

4Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, Münster, Germany

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Dina Robaa

5Institute of Pharmacy, Martin-Luther University of Halle-Wittenberg, Halle/Saale, Germany; and

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Wolfgang Sippl

5Institute of Pharmacy, Martin-Luther University of Halle-Wittenberg, Halle/Saale, Germany; and

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Roger Schibli

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

6Department of Nuclear Medicine, University Hospital Zurich, Zurich, Switzerland

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Bernhard Wünsch

4Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, Münster, Germany

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Linjing Mu

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

6Department of Nuclear Medicine, University Hospital Zurich, Zurich, Switzerland

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Simon M. Ametamey

1Institute of Pharmaceutical Sciences, ETH Zurich, Zurich, Switzerland

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Journal of Nuclear Medicine

Vol. 60, Issue 8

August 1, 2019

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Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-¹¹C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ₁-Receptor–Targeted PET Imaging

Journal of Nuclear Medicine Aug 2019, 60 (8) 1167-1173; DOI: 10.2967/jnumed.118.221051

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Journal of Nuclear Medicine Aug 2019, 60 (8) 1167-1173; DOI: 10.2967/jnumed.118.221051

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Keywords

PET imaging
GluN2B
σ1-receptor
receptor occupancy
neurodegeneration

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Preclinical Evaluation of Benzazepine-Based PET Radioligands (R)- and (S)-¹¹C-Me-NB1 Reveals Distinct Enantiomeric Binding Patterns and a Tightrope Walk Between GluN2B- and σ₁-Receptor–Targeted PET Imaging

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