title: Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
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.
authors.affiliation: Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Sweden.
authors.forename: B B
authors.initials: BB
authors.lastname: Höök
authors.forename: C
authors.initials: C
authors.lastname: Brege
authors.forename: T
authors.initials: T
authors.lastname: Linnanen
authors.forename: A
authors.initials: A
authors.lastname: Mikaels
authors.forename: A
authors.initials: A
authors.lastname: Malmberg
authors.forename: A M
authors.initials: AM
authors.lastname: Johansson
mesh_terms: D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D011869:Radioligand Assay; D013329:Structure-Activity Relationship; D013462:Sulfur Radioisotopes; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: C400302:2-((benzyl)propylamino)-5-methoxytetralin; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D013462:Sulfur Radioisotopes; D013764:Tetrahydronaphthalenes; D016244:Guanosine 5'-O-(3-Thiotriphosphate)