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

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4128-30. doi: 10.1016/j.bmcl.2007.05.057. Epub 2007 May 23.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Aporphines / chemistry
  • Aporphines / metabolism*
  • Ligands
  • Protein Binding
  • Rats
  • Receptor, Serotonin, 5-HT1A / metabolism*

Substances

  • Aporphines
  • Ligands
  • Receptor, Serotonin, 5-HT1A
  • aporphine