Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D₂ receptor

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• 作者：Hö ; ö ; k ; Berit Backlund ; Brege ; Cecilia ; Linnanen ; Tero ; Mikaels ; Å ; sa ; Malmberg ; Å ; sa ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1999
• 出版时间：August 2, 1999
• 年：1999
• 卷：9
• 期：15
• 页码：2167-2172
• 全文大小：282 K

文摘

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 characterized as a potent inverse agonists at DA D_2A receptors in a [³⁵S]GTPγS binding assay.