Investigation of an F-18 oxytocin receptor selective ligand via PET imaging
Open accessAbstract
The compound 1-(1-(2-(2-(2-fluoroethoxy)-4-(piperidin-4-yloxy)phenyl)acetyl)piperidin-4-yl)-3,4-dihydroquinolin-2(1H)-one (1) was synthesized and positively evaluated in vitro for high potency and selectivity with human oxytocin receptors. The positron emitting analogue, [F-18]1, was synthesized and investigated in vivo via PET imaging using rat and cynomolgus monkey models. PET imaging studies in female Sprague-Dawley rats suggested [F-18]1 reached the brain and accumulated in various regions of the brain, but washed out too rapidly for adequate quantification and localization. In vivo PET imaging studies in a male cynomolgus monkey suggested [F-18]1 had limited brain penetration while specific uptake of radioactivity significantly accumulated within the vasculature of the cerebral ventricles in areas representative of the choroid plexus.
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The authors' novel small-molecule OXTR antagonists failed to detect OXTR binding sites in vivo with PET.
“Unfortunately, these compounds have not been found useful for detecting OXTR binding sites in vivo using PET.”
From Comparative Perspectives on Oxytocin and Vasopressin Receptor Research in Rodents and Primates: Translational Implications (2016) · cites this paper as [92]
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References 29 · Cited by 28
Research works printed but not linked: 1
- [5]Insel TR Winslow JT Wang ZX Young L Hulihan TJ Adv. Exp. Med. Biol 1995 395 227 8713971
- Authors
- Smith, A. L., Freeman, S. M., Voll, R. J., Young, L. J., & Goodman, M. M.
- Affiliations
- Emory University (US)
- Emory National Primate Research Center (US)
- Corresponding author
- Young, Larry J.
- Goodman, Mark M.
- Venue
- Bioorganic & Medicinal Chemistry Letters
- Publisher
- Elsevier BV
- Published
- 2013-10
- Volume
- 23
- Issue
- 19
- Pages
- 5415-5420
- ISSN
- 0960-894X (ISSN-L)
- PMC
- PMC3955700
- OpenAlex
- W2069211121
- Cited by
- 28
- References
- 29
- Citations by year
- 2025: 1 · 2024: 1 · 2023: 1 · 2022: 1 · 2021: 1 · 2020: 2 · 2018: 2 · 2017: 4 · 2016: 8 · 2015: 3 · 2014: 4
- FWCI
- 3.87
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Bioorganic & Medicinal Chemistry Letters (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Institute of Mental Health (5 R21 MH090776)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Social Sciences › Psychology › Social Psychology › Neuroendocrine regulation and behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
- Keywords
- oxytocin receptor, positron emission tomography, radiotracer synthesis, brain penetration, choroid plexus, brain ventricles, receptor selectivity, Macaca fascicularis, rats
- MeSH terms
- Animals, Brain, Cells, Cultured, Chromatography, High Pressure Liquid, Female, Fluorine Radioisotopes, Humans, Ligands, Macaca fascicularis, Male, Rats, Sprague-Dawley, Receptors, Oxytocin, Models, Animal, Positron-Emission Tomography, Rats
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