2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl) methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D3 receptor

Article abstract of DOI:10.1016/S0960-894X(97)00045-0

A series of 2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles (8 - 15) has been prepared to investigate the effect on affinity and selectivity for the dopamine D₃ receptor of modifying the substituent in the phenyl ring at the 2-position of the pyrrole. Sulfonate 7 and sulfonamides 12, 14, 15 were shown to have high affinities (pKi's 8.0 - 8.7) and selectivities (100 - 150-fold) for the D₃ over the D₂ receptor.