Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D-2A receptor.

Authors
Hook, BB Brege, C Linnanen, T Mikaels, A Malmberg, A Johansson, AM
Citation
Bb. Hook et al., Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D-2A receptor., BIOORG MED, 9(15), 1999, pp. 2167-2172
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
15
Year of publication
1999
Pages
2167 - 2172
Database
ISI
SICI code
0960-894X(19990802)9:15<2167:DO(AAI>2.0.ZU;2-E
Abstract
A series of N-arylmethyl substituted (R)-5-methoxy-2-(propylamino)tetralins has been prepared and evaluated for affinity and efficacy at dopamine (DA) D-2A receptors. The novel compounds appeared to be antagonists or inverse agonists. (R)-2-[(Benzyl)propylamino]-5-methoxytetralin (7) was characteriz ed as a potent inverse agonists at DA D-2A receptors in a [S-35]GTP gamma S binding assay. (C) 1999 Elsevier Science Ltd. All rights reserved.