Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D-3 receptor

Authors
Austin, NE Avenell, KY Boyfield, I Branch, CL Hadley, MS Jeffrey, P Johnson, CN Macdonald, GJ Nash, DJ Riley, GJ Smith, AB Stemp, G Thewlis, KM Vong, AKK Wood, M
Citation
Ne. Austin et al., Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D-3 receptor, BIOORG MED, 10(22), 2000, pp. 2553-2555
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
22
Year of publication
2000
Pages
2553 - 2555
Database
ISI
SICI code
0960-894X(20001120)10:22<2553:N2WHAA>2.0.ZU;2-B
Abstract
Starting from the dopamine D-3 receptor antagonist SE-277011 1, a series of 2,3,4,5-tetrahydro-1H-3-benzazepines has been identified with high affinit y for the dopamine D3 receptor and selectivity over the D-2 receptor. The 3 -acetamido-2-fluorocinnamide derivative 20 gave high D-3 receptor affinity (pK(i) 8.4) with 130-fold selectivity over the D-2 receptor. (C) 2000 Elsev ier Science Ltd. All rights reserved.