Novel cyclohexyl amides as potent and selective D3 dopamine receptor ligands
The dopamine D3 receptor is an attractive target for the treatment of schizophrenia. We identified PD137557 (V) as a ligand for the D2 receptor and desired to prepare a selective D3 compound. SAR studies involving different amides and different phenyl piperazines have led to the discovery of 8a and 8c as selective D3 receptor ligands.
Belliotti, Thomas R.,Kesten, Suzanne R.,Rubin, John R.,Wustrow, David J.,Georgic, Lynn M.,Zoski, Kim T.,Akunne, Hyacinth C.,Wise, Lawrence D.