Synthesis and evaluation of 3-123I-iodo-5-[2-(S)-3-pyrrolinylmethoxy]-pyridine (niodene) as a potential nicotinic α4β2 receptor imaging agent
| Autor: | Ritu Kant, Suresh K. Pandey, Jogeshwar Mukherjee, Shawn Pan, Sharon Kuruvilla, Min-Liang Pan |
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| Rok vydání: | 2012 |
| Předmět: |
Chemistry
Organic Chemistry Clinical Biochemistry Pharmaceutical Science Nifene Pharmacology Biochemistry Imaging agent Nicotine Nicotinic agonist Spect imaging Drug Discovery medicine Molecular Medicine Alpha-4 beta-2 nicotinic receptor Receptor Molecular Biology medicine.drug Acetylcholine receptor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 22:7610-7614 |
| ISSN: | 0960-894X |
| Popis: | Nicotinic acetylcholine receptors (nAChRs) are downregulated in disease conditions such as Alzheimer's and substance abuse. Presently, (123)I-5-IA-85380 is used in human studies and requires over 6h of scanning time, thus increases patient discomfort. We have designed and synthesized 3-iodo-5-[2-(S)-3-pyrrolinylmethoxy]pyridine (niodene) with the aim to have faster binding kinetics compared to (123)I-5-IA-85380, which may reduce scanning time and help in imaging studies. Binding affinity K(i) of niodene for rat brain α4β2 receptors in brain homogenate assays using (3)H-cytisine was 0.27 nM. Niodene, 10nM displaced >95% of (18)F-nifene bound to α4β2 receptors in rat brain slices. By using the iododestannylation method, (123)I-niodene was obtained in high radiochemical purity (>95%) but with low radiochemical yield ( |
| Databáze: | OpenAIRE |
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