A NOVEL SERIES OF 2-AMINOTETRALINS WITH HIGH-AFFINITY AND SELECTIVITYFOR THE DOPAMINE D-3 RECEPTOR

Authors
BOYFIELD I COLDWELL MC HADLEY MS JOHNSON CN RILEY GJ SCOTT EE STACEY R STEMP G THEWLIS KM
Citation
I. Boyfield et al., A NOVEL SERIES OF 2-AMINOTETRALINS WITH HIGH-AFFINITY AND SELECTIVITYFOR THE DOPAMINE D-3 RECEPTOR, Bioorganic & medicinal chemistry letters, 7(15), 1997, pp. 1995-1998
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
15
Year of publication
1997
Pages
1995 - 1998
Database
ISI
SICI code
0960-894X(1997)7:15<1995:ANSO2W>2.0.ZU;2-S
Abstract
A novel series of ylamino)butyl]-1,2,3,4-tetrahydro-2-naphthylamines w ith high affinity and selectivity for the dopamine D-3 receptor has be en prepared. The 5-cyclopropylmethyloxy 3j, methanesulfonyloxy 3k and trifluoromethanesulfonyloxy 3l derivatives represent some of the highe st affinity (pKi's 8.6-8.9) and most selective (200-320-fold) dopamine D-3 receptor antagonists reported to date. (C) 1997 Elsevier Science Ltd.