alexa R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.


Medicinal Chemistry

Author(s): Si YG, Gardner MP, Tarazi FI, Baldessarini RJ, Neumeyer JL

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Abstract Several N-substituted-11-hydroxy-10-hydroxymethyl- and 11-hydroxy-10-methylaporphines were synthesized and their binding affinities at dopamine D(1) and D(2) receptors and serotonin 5-HT(1A) and 5-HT(2A) receptors in rat forebrain tissue were evaluated. Tested compounds displayed moderate to high affinity to 5-HT(1A) receptors but low affinity to D(1) and D(2) receptors. The most potent novel 5-HT(1A) agent was R-(-)-N-methyl-10-hydroxymethyl-11-hydroxyaporphine. This article was published in Bioorg Med Chem Lett and referenced in Medicinal Chemistry

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