Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1398992 | European Journal of Medicinal Chemistry | 2013 | 13 Pages |
•Synthesis of 11 novel analogs of l-prolyl-l-leucylglycinamide (PLG).•The prolyl residue of PLG was replaced by a 3,5-disubstituted proline scaffold.•These analogs were tested as allosteric modulators of dopamine D2 receptors.•Compounds 18b and 19b increased [3H] NPA binding at concentrations of 10−12–10−9 M.
Novel analogs of l-prolyl-l-leucylglycinamide (PLG) were synthesized wherein the prolyl residue was replaced with other amino acids based on a 3,5-disubstituted proline scaffold. In some examples, the l-leucyl residue was also replaced by l-valine. These analogs were tested for their ability to enhance the binding of [3H]-N-propylnorapomorphine to short isoform of human dopamine D2 receptors.Compounds 18b and 19b, increased [3H] NPA binding at concentrations between 10−12 and 10−9 M, which is similar to the effect of PLG in this assay and, provides evidences that these compounds are acting as allosteric modulators of dopamine D2 receptors.
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