Please use this identifier to cite or link to this item: http://ahro.austin.org.au/austinjspui/handle/1/12906
Title: Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists.
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
Citation: 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.
Internal ID Number: 2963964
URI: http://ahro.austin.org.au/austinjspui/handle/1/12906
URL: http://www.ncbi.nlm.nih.gov/pubmed/2963964
Type: Journal Article
Subjects: Animals
Binding, Competitive
Chemical Phenomena
Chemistry
Corpus Striatum.metabolism
Guanosine Triphosphate.pharmacology
Male
Naphthalenes.pharmacology
Phenethylamines.pharmacology
Radioligand Assay
Rats
Rats, Inbred Strains
Receptors, Dopamine.drug effects.metabolism
Receptors, Dopamine D2
Spiperone.metabolism
Tetrahydronaphthalenes.pharmacology
Thiophenes.pharmacology
Appears in Collections:Journal articles

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