Biodistribution and dosimetry of ¹²³I-mZIENT: a novel ligand for imaging serotonin transporters

Nicol, A., Krishnadas, R. , Champion, S. , Tamagnan, G., Stehouwer, J.S., Goodman, M.M., Hadley, D. and Pimlott, S.L. (2012) Biodistribution and dosimetry of ¹²³I-mZIENT: a novel ligand for imaging serotonin transporters. European Journal of Nuclear Medicine and Molecular Imaging, 39(5), pp. 786-791. (doi: 10.1007/s00259-011-2056-x)

Abstract

Purpose: ¹²³I-labelled mZIENT (2β-carbomethoxy-3β-(3′-((Z)-2-iodoethenyl)phenyl)nortropane) has been developed as a radioligand for the serotonin transporter. The aim of this preliminary study was to assess its whole-body biodistribution in humans and estimate dosimetry. <p/>Methods: Three healthy controls and three patients receiving selective serotonin reuptake inhibitor (SSRI) therapy for depression were included (two men, four women, age range 41–56 years). Whole-body imaging, brain SPECT imaging and blood and urine sampling were performed. Whole-body images were analysed using regions of interest (ROIs), time–activity curves were derived using compartmental analysis and dosimetry estimated using OLINDA software. Brain ROI analysis was performed to obtain specific-to-nonspecific binding ratios in the midbrain, thalamus and striatum. <p/>Results: Initial high uptake in the lungs decreased in later images. Lower uptake was seen in the brain, liver and intestines. Excretion was primarily through the urinary system. The effective dose was estimated to be of the order of 0.03 mSv/MBq. The organ receiving the highest absorbed dose was the lower large intestine wall. Uptake in the brain was consistent with the known SERT distribution with higher specific-to-nonspecific binding in the midbrain, thalamus and striatum in healthy controls compared with patients receiving SSRI therapy. <p/>Conclusion: ¹²³I-mZIENT may be a promising radioligand for imaging the serotonin transporters in humans with acceptable dosimetry.

• Item Type: Articles
• Status: Published
• Refereed: Yes
• Glasgow Author(s) Enlighten ID: Pimlott, Dr Sally and Champion, Dr Sue and Krishnadas, Dr Rajeev and Hadley, Professor Donald and Nicol, Dr Alice
• Authors: Nicol, A., Krishnadas, R., Champion, S., Tamagnan, G., Stehouwer, J.S., Goodman, M.M., Hadley, D., and Pimlott, S.L.
• College/School: College of Medical Veterinary and Life Sciences > School of Psychology & Neuroscience; College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing; College of Medical Veterinary and Life Sciences > School of Health & Wellbeing > Mental Health and Wellbeing
• Journal Name: European Journal of Nuclear Medicine and Molecular Imaging
• ISSN: 1619-7070
• Published Online: 03 February 2012