]-5-[1-(2-PHENYLAZACYCLOHEPTYL)METHYL]-1H-PYRROLES WITH HIGH-AFFINITYAND SELECTIVITY FOR THE DOPAMINE D-3 RECEPTOR

Authors
BOLTON D BOYFIELD I COLDWELL MC HADLEY MS JOHNS A JOHNSON CN MARKWELL RE NASH DJ RILEY GJ SCOTT EE SMITH SA STEMP G WADSWORTH HJ WATTS EA
Citation
D. Bolton et al., ]-5-[1-(2-PHENYLAZACYCLOHEPTYL)METHYL]-1H-PYRROLES WITH HIGH-AFFINITYAND SELECTIVITY FOR THE DOPAMINE D-3 RECEPTOR, Bioorganic & medicinal chemistry letters, 7(4), 1997, pp. 485-488
Citations number
8
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
4
Year of publication
1997
Pages
485 - 488
Database
ISI
SICI code
0960-894X(1997)7:4<485:]WH>2.0.ZU;2-Z
Abstract
A series of ]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles (8 - 15 ) has been prepared to investigate the effect on affinity and selectiv ity for the dopamine Dg receptor of modifying the substituent in the p henyl ring at the 2-position of the pyrrole. Sulfonate 7 and sulfonami des 12, 14, 15 were shown to have high affinities (pKi's 8.0 - 8.7) an d selectivities (100 - 150-fold) for the D-3 over the D-2 receptor. (C ) 1997, Elsevier Science Ltd.