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Molecular Imaging and Biology
Published in: Molecular Imaging and Biology 3/2007

01-05-2007 | Research Article

In Vivo DA D1 Receptor Selectivity of NNC 112 and SCH 23390

Authors: Jesper Ekelund, Mark Slifstein, Raj Narendran, Olivier Guillin, Hemant Belani, Ning-Ning Guo, Yuying Hwang, Dah-Ren Hwang, Anissa Abi-Dargham, Marc Laruelle

Published in: Molecular Imaging and Biology | Issue 3/2007

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Abstract

Purpose

[11C]NNC 112 and [11C]SCH 23390 are selective positron emission tomography (PET) tracers for visualizing dopamine D1 receptors. It is known that both have some affinity for serotonin 2A receptors, but previous studies have suggested this is negligible compared to D1 affinity. We sought to verify this property in vivo.

Procedures

Two baboons were scanned to measure the selectivity of both tracers with a displacement paradigm. Four baboons were scanned to directly assess [11C] NNC 112 affinity for both receptors.

Results

In vivo, D1 to 5-HT2A selectivity is six to fourteenfold, not 100-fold as previously reported by other investigators.

Conclusion

We conclude that about 1/4 of the cortical signal of both [11C]NNC 112 and [11C]SCH 23390 is due to binding to 5-HT2A receptors. If confirmed in humans, this suggests caution should be exercised when drawing conclusions from studies using either tracer. These results also indicate the need for more selective tracers for the D1 receptor.
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Metadata
Title
In Vivo DA D1 Receptor Selectivity of NNC 112 and SCH 23390
Authors
Jesper Ekelund
Mark Slifstein
Raj Narendran
Olivier Guillin
Hemant Belani
Ning-Ning Guo
Yuying Hwang
Dah-Ren Hwang
Anissa Abi-Dargham
Marc Laruelle
Publication date
01-05-2007
Publisher
Springer-Verlag
Published in
Molecular Imaging and Biology / Issue 3/2007
Print ISSN: 1536-1632
Electronic ISSN: 1860-2002
DOI
https://doi.org/10.1007/s11307-007-0077-4

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