Add time:09/05/2019 Source:sciencedirect.com
We prepared 5-HT1A receptor ligands (S)-N-{[1-(2-phenylethyl)pyrrolidin-2-yl]methyl}-3-[11C]methylthiobenzamide ([11C](S)-PPMMB) (Ki = 4.3 nM) and the less active [11C](R)-PPMMB (Ki = 160 nM) by reduction of the disulfide dimer and subsequent [11C]methylation of demethyl (S)- and (R)-PPMMB, respectively. Both radioligands showed similar brain distribution in mice with relatively higher affinity for the hippocampus being rich in 5-HT1A receptors than for other brain regions. Uptake of [11C](S)-PPMMB was not reduced by carrier-loading nor by pretreatment with 5-HT1A receptor ligands. [11C](S)-PPMMB is therefore not a suitable radioligand for mapping 5-HT1A receptors using positron emission tomography.
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