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

✍ Scribed by David Bolton; Izzy Boyfield; Martyn C. Coldwell; Michael S. Hadley; Amanda Johns; Christopher N. Johnson; Roger E. Markwell; David J. Nash; Graham J. Riley; Emma E. Scott; Stephen A. Smith; Geoffrey Stemp; Harry J. Wadsworth; Eric A. Watts

Publisher: Elsevier Science
Year: 1997
Tongue: English
Weight: 192 KB
Volume: 7
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(97)00045-0

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✦ Synopsis

A series of 2-1(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-lH-pyrroles (8 -15) has been prepared to investigate the effect on affinity and selectivity for the dopamine D 3 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 (10(I -150-fold) for the D 3 over the D 2 receptor.

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