Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.

Article Details

Citation

van Vliet LA, Tepper PG, Dijkstra D, Damsma G, Wikstrom H, Pugsley TA, Akunne HC, Heffner TG, Glase SA, Wise LD

Affinity for dopamine D2, D3, and D4 receptors of 2-aminotetralins. Relevance of D2 agonist binding for determination of receptor subtype selectivity.

J Med Chem. 1996 Oct 11;39(21):4233-7.

PubMed ID
8863800 [ View in PubMed
]
Abstract

A series of 2-aminotetralins, substituted with a methoxy or a hydroxy group on the 5- or 7-position, and with varying N-alkyl or N-arylalkyl substituents, were prepared and evaluated in binding assays for human dopamine (DA) D2, D3, and D4 receptors. Some members of this series were prepared in former studies, but were never tested in vitro with single receptor subtypes, and these were examined again. None of the tested 2-aminotetralins showed high affinity for the dopamine D4 receptor. However, a number of the 2-aminotetralins showed high affinity for both the D2 and the D3 DA receptors, as exemplified by compounds 11-15 and 21-26, while some had a reasonable selectivity for the DA D3 receptors. The affinities of the 2-aminotetralins for the D21, receptor depended on the type of radioligand (agonist or antagonist) used. The agonist affinity data, obtained by using the agonist ligand [3H]N-0437, are thought to be more relevant for calculating DA receptor subtype selectivity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RotigotineDopamine D2 receptorKi (nM)20N/AN/ADetails
RotigotineDopamine D2 receptorKi (nM)0.06N/AN/ADetails
RotigotineDopamine D3 receptorKi (nM)4N/AN/ADetails
RotigotineDopamine D4 receptorKi (nM)55N/AN/ADetails