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Title: Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists.
Austin Authors: Beart, P M;Cook, C J;Cincotta, M;de Vries, D J;Tepper, P;Dijkstra, D;Horn, A S
Affiliation: University of Melbourne, Clinical Pharmacology and Therapeutics Unit, Austin Hospital, Heidelberg, Victoria, Australia
Issue Date: 1-Nov-1987
Publication information: Naunyn-schmiedeberg's Archives of Pharmacology; 336(5): 487-93
Abstract: The affinity of a series of N,N-disubstituted 2-aminotetralins for the rat striatal D2 dopamine receptor labelled by [3H]spiperone has been determined. Displacement data for the more potent 2-aminotetralins were better described by a model where the compounds competed for [3H]spiperone at two sites. The high affinity component accounted for approximately 80% of the total sites. Displacement curves for all 2-aminotetralins were shifted to the right by 100 microM guanosine-5'-triphosphate; a result attributable to the redistribution of 13-47% of the sites to a low affinity form. These data are consistent with the N,N-disubstituted 2-aminotetralins being agonists at the D2 dopamine receptor. In particular, the affinities of the 5-hydroxy-2-aminotetralins were as high as those of traditional dopamine agonists.
Gov't Doc #: 2963964
Journal: Naunyn-Schmiedeberg's archives of pharmacology
Type: Journal Article
Subjects: Animals
Binding, Competitive
Chemical Phenomena
Corpus Striatum.metabolism
Guanosine Triphosphate.pharmacology
Radioligand Assay
Rats, Inbred Strains
Receptors, Dopamine.drug effects.metabolism
Receptors, Dopamine D2
Appears in Collections:Journal articles

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