Derivatives of (R)-2-amino-5-methoxytetralin: antagonists and inverse agonists at the dopamine D2A receptor.
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.
Höök
B B
BB
Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Sweden.
Brege
C
C
Linnanen
T
T
Mikaels
A
A
Malmberg
A
A
Johansson
A M
AM
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
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)