Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor

B B Höök; C Brege; T Linnanen; A Mikaels; A Malmberg; A M Johansson

doi:10.1016/s0960-894x(99)00345-5

Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor

Bioorg Med Chem Lett. 1999 Aug 2;9(15):2167-72. doi: 10.1016/s0960-894x(99)00345-5.

Authors

B B Höök¹, C Brege, T Linnanen, A Mikaels, A Malmberg, A M Johansson

Affiliation

¹ Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Sweden.

PMID: 10465538
DOI: 10.1016/s0960-894x(99)00345-5

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) D2A 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 D2A receptors in a [35S]GTPgammaS binding assay.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Dopamine Antagonists / chemical synthesis*
Dopamine Antagonists / chemistry
Dopamine Antagonists / pharmacology
Dopamine D2 Receptor Antagonists*
Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
Humans
Radioligand Assay
Structure-Activity Relationship
Sulfur Radioisotopes
Tetrahydronaphthalenes / chemical synthesis*
Tetrahydronaphthalenes / pharmacology

Substances

2-((benzyl)propylamino)-5-methoxytetralin
Dopamine Antagonists
Dopamine D2 Receptor Antagonists
Sulfur Radioisotopes
Tetrahydronaphthalenes
Guanosine 5'-O-(3-Thiotriphosphate)