Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.
Basic Information
ID: ALA1139330
Journal: Bioorg Med Chem Lett
Title: Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.
Authors: Si YG, Choi YK, Gardner MP, Tarazi FI, Baldessarini RJ, Neumeyer JL.
Abstract: We synthesized several esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines, assessed their affinities at dopamine D(1) and D(2) receptors in rat forebrain tissue and quantified their effects on motor activity in normal adult male rats. Tested compounds displayed moderate to high affinities to D(2) receptors but low affinities to D(1) receptors. The most D(2)-potent (K(i)=18.9nM) and selective novel agent (>529-fold vs D(1) sites) was R(-)-2-methoxy-11-acetyloxy-N-n-propylnoraporphine (compound 4b). At moderate doses, the compound proved to have prolonged behavioral locomotor activity.
CiteXplore: 19058967
DOI: 10.1016/j.bmcl.2008.11.025
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