Novel cyclohexyl amides as potent and selective D 3 dopamine receptor ligands

…, SR Kesten, JR Rubin, DJ Wustrow, LM Georgic…

Index: Belliotti, Thomas R.; Kesten, Suzanne R.; Rubin, John R.; Wustrow, David J.; Georgic, Lynn M.; Zoski, Kim T.; Akunne, Hyacinth C.; Wise, Lawrence D. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 18 p. 2403 - 2408

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Citation Number: 24

Abstract

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.