Evaluation of Carbon-11-Labeled 2β-Carbomethoxy-3β-[4‘-((Z)-2-iodoethenyl)phenyl]nortropane as a Potential Radioligand for Imaging the Serotonin Transporter by PET

The nortropane cocaine analogue, 2β-carbomethoxy-3β-[4‘-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Synthesis of t...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2006-02, Vol.49 (3), p.942-946
Main Authors: Plisson, Christophe, Jarkas, Nachwa, McConathy, Jon, Voll, Ronald J, Votaw, John, Williams, Larry, Howell, Leonard L, Kilts, Clinton D, Goodman, Mark M
Format: Article
Language:English
Subjects:
Biological and medical sciences
Contrast media. Radiopharmaceuticals
Medical sciences
Pharmacology. Drug treatments
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Summary:The nortropane cocaine analogue, 2β-carbomethoxy-3β-[4‘-((Z)-2-iodoethenyl)phenyl]nortropane (ZIENT), is a high affinity, selective serotonin transporter (SERT) ligand that has shown promise as a SERT imaging agent for single photon computed tomography (SPECT) when labeled with I-123. Synthesis of the labeling precursor, radiosynthesis of [11C]ZIENT, and in vivo evaluation in anesthetized and awake monkeys have been performed to determine the suitability of [11C]ZIENT as a PET agent for SERT imaging.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm050799v