| Autor: |
Misato, Takashima-Hirano, Syusaku, Tazawa, Kazuhiro, Takahashi, Hisashi, Doi, Masaaki, Suzuki |
| Rok vydání: |
2011 |
| Předmět: |
|
| Zdroj: |
Chemicalpharmaceutical bulletin. 59(8) |
| ISSN: |
1347-5223 |
| Popis: |
Ramelteon (TAK-375) is a novel melatonin receptor agonist that is used for clinical treatment of insomnia. The present report describes radiolabeling of ramelteon with the short-lived positron-emitter ¹¹C (T(1/2)=20.4 min) by 2 methods. One method was [¹¹C]methylation of an acetoamide precursor and the other was [¹¹C]acylation of the corresponding amine precursor. First, [¹¹C]methylation method showed the low reproducibility together with the production of many kinds of side products from which the [¹¹C-methyl]Ramelteon was separated with chemical purity of28% and radiochemical purity of98%. Whereas, the [¹¹C]acylation method showed high efficiency and reproducibility with a good radiochemical yield (22-43%, decay corrected), high chemical and radiochemical purities (99% each), and high specific activity (43-162 GBq/µmol) (n=5) after HPLC purification. [¹¹C]Ramelteon is a potential positron emission tomography (PET) probe for imaging the melatonin receptor. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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