guanosine-triphosphate and 2-aminotetralin

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.

Topics: Animals; Binding, Competitive; Chemical Phenomena; Chemistry; Corpus Striatum; Guanosine Triphosphate; Male; Naphthalenes; Phenethylamines; Radioligand Assay; Rats; Rats, Inbred Strains; Receptors, Dopamine; Receptors, Dopamine D2; Spiperone; Tetrahydronaphthalenes; Thiophenes