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Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor

✍ Scribed by David Bolton; Izzy Boyfield; Martyn C. Coldwell; Michael S. Hadley; Maureen A.M. Healy; Christopher N. Johnson; Roger E. Markwell; David J. Nash; Graham J. Riley; Geoffrey Stemp; Harry J. Wadsworth

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 175 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00202-8

No coin nor oath required. For personal study only.

✦ Synopsis

A series of 2,5-disubstituted-1H-pyrroles (4-18) has been prepared based on replacement of the amide of sultopride 1 by a pyrrole ring. Subsequent modification of the basic side chain gave compounds with high affinity for the dopamine D3 receptor. In addition, 12 and 17 were shown to be D3 antagonists with 30-fold selectivity for the D3 receptor over the D2 receptor.

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