Autor: |
Tanaka A, Okano K, Tamagami H, Matsumoto H, Tanifuji S, Yamamichi Y, Yoshimura H, Makoto AZUMA, Ph.D., Takano K, Matsumura K, Takeda K |
Rok vydání: |
1999 |
Předmět: |
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Zdroj: |
Europe PubMed Central |
ISSN: |
0022-7854 |
Popis: |
The metabolism of N-(3-fluoropropyl)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)nortropane (123I) (123I-FP-CIT) in healthy humans was studied. Plasma and urine samples, obtained after i.v. administration of 123I-FP-CIT, were analyzed using the two-dimensional thin-layer chromatography technique. Eleven radiochemical components were detected in both plasma and urine, and four of them were the parent 123I-FP-CIT and its metabolites, N-(3-fluoropropyl)-2 beta-carboxy-3 beta-(4-iodophenyl)nortropane (123I) (123I-acid), 2 beta-carboxy-3 beta-(4-iodophenyl)nortropane (123I) (123I-nor-acid) and 2 beta-carbomethoxy-3 beta-(4-iodophenyl)nortropane (123I) (123I-nor-CIT). These four identified radiochemical components occupied about 80% or more in ratio of the radiochemical components in the plasma and urine. In the metabolites of 123I-FP-CIT, the high polar metabolites--123I-acid and 123I-nor-acid--were found to be the major components, while lipophilic 123I-nor-CIT was a minor component. Free iodide (123I-) was not found in the plasma or urine. Thus, the main metabolic reactions which 123I-FP-CIT undergoes in humans seem to be hydrolysis of the ester bond and N-dealkylation. In vivo deiodination of 123I-FP-CIT was found to be minimum. Current results suggest that the metabolites of 123I-FP-CIT hardly influence evaluation of the dopamine transporter in the human brain. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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