Journal article

RADIORECEPTOR BINDING REVEALS THE POTENCIES OF N,N-DISUBSTITUTED 2-AMINOTETRALINS AS D2 DOPAMINE AGONISTS

PM BEART, CJ COOK, M CINCOTTA, DJ DEVRIES, P TEPPER, D DIJKSTRA, AS HORN

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY | SPRINGER | Published : 1987

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..

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