caa a22 4500 378907255 CHVBK 20180305123533.0 cr unu---uuuuu 161128e20040401xx s 000 0 eng 10.1524/ract.92.4.345.35592 doi (NATIONALLICENCE)gruyter-10.1524/ract.92.4.345.35592 Radiosynthesis and in vitro evaluation of the 5HT2 receptor ligand [N-11C-methyl]-1-[2,5-dimethoxy-4-iodophenyl]-2-methylaminopropane for PET [Elektronische Daten] [J. Schmaljohann, A. Becherer, K. Kletter, D. Gündisch] 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. © 2004 Oldenbourg Wissenschaftsverlag GmbH Laboratory techniques, experiments nationallicence Analytical chemistry nationallicence Inorganic chemistry nationallicence Schmaljohann J. aut Becherer A. aut Kletter K. aut Gündisch D. aut Radiochimica Acta/International journal for chemical aspects of nuclear science and technology Oldenbourg Wissenschaftsverlag GmbH 92/4-6/2004(2004-04-01), 345-348 0033-8230 92:4-6/2004<345 2004 92 ract https://doi.org/10.1524/ract.92.4.345.35592 text/html Onlinezugriff via DOI 1 research article jats NATIONALLICENCE 856 40 https://doi.org/10.1524/ract.92.4.345.35592 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Schmaljohann J. aut NATIONALLICENCE 700 1- Becherer A. aut NATIONALLICENCE 700 1- Kletter K. aut NATIONALLICENCE 700 1- Gündisch D. aut NATIONALLICENCE 773 0- Radiochimica Acta/International journal for chemical aspects of nuclear science and technology Oldenbourg Wissenschaftsverlag GmbH 92/4-6/2004(2004-04-01), 345-348 0033-8230 92:4-6/2004<345 2004 92 ract CC0 http://creativecommons.org/publicdomain/zero/1.0 nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-gruyter