Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor

Hindered rotation analogs of the antipsychotic mazapertine (1) were prepared. These compounds exhibited high affinity for the HT-1A receptor, but not for other serotonin or dopamine receptors. The related β-carboline structures were also sybthetized and were found to be potent 5-HT1A ligands.