Affinity for dopamine D-2, D-3, and D-4 receptors of 2-aminotetralins. Relevance of D-2 agonist binding for determination of receptor subtype selectivity

L A vanVliet*, P G Tepper, D Dijkstra, G Damsma, H Wikstrom, TA Pugsley, HC Akunne, TG Heffner, SA Glase, LD Wise

*Corresponding author for this work

    Research output: Contribution to journalArticleAcademicpeer-review

    58 Citations (Scopus)

    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) D-2, D-3, and D-4 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 D-4 receptor. However, a number of the 2-aminotetralins showed high affinity for both the D-2 and the D-3 DA receptors, as exemplified by compounds 11-15 and 21-26, while some had a reasonable selectivity for the DA D-3 receptors. The affinities of the 2-aminotetralins for the D-2L receptor depended on the type of radioligand (agonist or antagonist) used. The agonist affinity data, obtained by using the agonist ligand [H-3]N-0437, are thought to be more relevant for calculating DA receptor subtype selectivity.

    Original languageEnglish
    Pages (from-to)4233-4237
    Number of pages5
    JournalJournal of Medicinal Chemistry
    Volume39
    Issue number21
    DOIs
    Publication statusPublished - 11-Oct-1996

    Keywords

    • STRUCTURAL REQUIREMENTS
    • D3
    • SCHIZOPHRENIA
    • DERIVATIVES
    • SERIES
    • STATES
    • SITES
    • MONOHYDROXYAMINOTETRALINS
    • 2-AMINOTETRALINS
    • IDENTIFICATION

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