170288-10-5Relevant articles and documents
2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl) methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D3 receptor
Bolton, David,Boyfield, Izzy,Coldwell, Martyn C.,Hadley, Michael S.,Johns, Amanda,Johnson, Christopher N.,Markwell, Roger E.,Nash, David J.,Riley, Graham J.,Scott, Emma E.,Smith, Stephen A.,Stemp, Geoffrey,Wadsworth, Harry J.,Watts, Eric A.
, p. 485 - 488 (1997)
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.