McN5652

McN5652 is a molecule that can be radiolabeled and then used as a radioligand in positron emission tomography (PET) studies. The &#91;11C&#93;-(+)-McN5652 enantiomer binds to the serotonin transporter. The radioligand is used for molecular neuroimaging and for imaging of the lungs.

It was developed by Johnson & Johnson's McNeil Laboratories. According to McNeil, McN5652 was among the strongest SRI ever reported at the time of its discovery (sub nM Ki). However, it is not completely 5-HT selective: the racemate has 5-HT=0.68, NA=2.9, and D=36.8nM, whereas (+)-enantiomer has 5-HT=0.39, NA=1.8, and D=23.5 nM. Paroxetine was listed as 5-HT=0.44 nM, NA=20, and DA=460nM in the same paper by the same authors.

Derivatives
McN5652 and related structures have been analyzed for QSAR in terms of binding to the MAT receptor binding site.