Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists.
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.
D000818:Animals; D001667:Binding, Competitive; D055598:Chemical Phenomena; D002621:Chemistry; D003342:Corpus Striatum / Q000378:metabolism; D006160:Guanosine Triphosphate / Q000494:pharmacology; D008297:Male; D009281:Naphthalenes / Q000494:pharmacology*; D010627:Phenethylamines / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D011919:Rats, Inbred Strains; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000378:metabolism; D017448:Receptors, Dopamine D2; D013134:Spiperone / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000494:pharmacology*; D013876:Thiophenes / Q000494:pharmacology
D009281:Naphthalenes; D010627:Phenethylamines; D011954:Receptors, Dopamine; D017448:Receptors, Dopamine D2; D013764:Tetrahydronaphthalenes; D013876:Thiophenes; C006561:2-aminotetralin; D013134:Spiperone; D006160:Guanosine Triphosphate; C041369:2-(N-phenethyl-N-propyl)amino-5-hydroxytetralin; C047508:rotigotine