Synthesis and evaluation of 11C-labeled (S)-N-{[1-(2-phenylethyl) pyrrolidin-2-yl]methyl}-3-methylthiobenzamide as a PET 5-HT1A receptor ligand

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.

We also recommend Trading Suppliers and Manufacturers of (R)-2,2-diphenyl-2-(pyrrolidin-3-yl)acetonitrile (cas 133099-12-4). Pls Click Website Link as below: cas 133099-12-4 suppliers

Prev:Research paperNovel routes to either racemic or enantiopure α-amino-(4-hydroxy-pyrrolidin-3-yl)acetic acid derivatives and biological evaluation of a new promising pharmacological scaffold
Next:Enantiospecific and diastereoselective synthesis of 4,4-disubstituted-3-amino-2-azetidinones, starting from D-serine)