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|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.|
|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|
Rats, Inbred Strains
Receptors, Dopamine.drug effects.metabolism
Receptors, Dopamine D2
|Appears in Collections:||Journal articles|
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