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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 | URI: | http://ahro.austin.org.au/austinjspui/handle/1/12906 | Journal: | Naunyn-Schmiedeberg's archives of pharmacology | URL: | https://pubmed.ncbi.nlm.nih.gov/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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