Radiosynthesis and in vitro evaluation of the 5HT2 receptor ligand [N-11C-methyl]-1-[2,5-dimethoxy-4-iodophenyl]-2-methylaminopropane for PET

Verfasser / Beitragende:
[J. Schmaljohann, A. Becherer, K. Kletter, D. Gündisch]
Ort, Verlag, Jahr:
2004
Enthalten in:
Radiochimica Acta/International journal for chemical aspects of nuclear science and technology, 92/4-6/2004(2004-04-01), 345-348
Format:
Artikel (online)
ID: 378907255
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024 7 0 |a 10.1524/ract.92.4.345.35592  |2 doi 
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245 0 0 |a Radiosynthesis and in vitro evaluation of the 5HT2 receptor ligand [N-11C-methyl]-1-[2,5-dimethoxy-4-iodophenyl]-2-methylaminopropane for PET  |h [Elektronische Daten]  |c [J. Schmaljohann, A. Becherer, K. Kletter, D. Gündisch] 
520 3 |a In vivo labelling of serotonergic receptors (5HT) could be a useful tool for understanding the physiological and pathophysiological role of neurodegenerative disorders. 1-[2,5-Dimethoxy-4-iodophenyl]-2-aminopropane (DOI), a well known agonist with high affinity to 5HT2 receptors, was labelled with C-11 for PET. Here we report the evaluation of the mono-methylated and dimethylated analogs of DOI for PET. The syntheses of [N-11C-methyl]-DOI ([11C]MDOI) and [N-11C-dimethyl]-DOI ([11C]DMDOI) were optimized resulting in radiochemical yields of up to 43%, allowing efficient production for clinical use. High affinities for the 5HT2A and 5HT2C receptors with a slight preference for 5HT2A were found for MDOI, similar to the highly potent hallucinogen DOI. 
540 |a © 2004 Oldenbourg Wissenschaftsverlag GmbH 
690 7 |a Laboratory techniques, experiments  |2 nationallicence 
690 7 |a Analytical chemistry  |2 nationallicence 
690 7 |a Inorganic chemistry  |2 nationallicence 
700 1 |a Schmaljohann  |D J.  |4 aut 
700 1 |a Becherer  |D A.  |4 aut 
700 1 |a Kletter  |D K.  |4 aut 
700 1 |a Gündisch  |D D.  |4 aut 
773 0 |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology  |d Oldenbourg Wissenschaftsverlag GmbH  |g 92/4-6/2004(2004-04-01), 345-348  |x 0033-8230  |q 92:4-6/2004<345  |1 2004  |2 92  |o ract 
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950 |B NATIONALLICENCE  |P 700  |E 1-  |a Schmaljohann  |D J.  |4 aut 
950 |B NATIONALLICENCE  |P 700  |E 1-  |a Becherer  |D A.  |4 aut 
950 |B NATIONALLICENCE  |P 700  |E 1-  |a Kletter  |D K.  |4 aut 
950 |B NATIONALLICENCE  |P 700  |E 1-  |a Gündisch  |D D.  |4 aut 
950 |B NATIONALLICENCE  |P 773  |E 0-  |t Radiochimica Acta/International journal for chemical aspects of nuclear science and technology  |d Oldenbourg Wissenschaftsverlag GmbH  |g 92/4-6/2004(2004-04-01), 345-348  |x 0033-8230  |q 92:4-6/2004<345  |1 2004  |2 92  |o ract 
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