Mazapertine (RWJ-37796) is an antipsychotic agent that was developed by Johnson & Johnson but never marketed. It exerts its pharmacological effect through affinity for dopamine D2, serotonin 5-HT1A, and α1-adrenergic receptors. Mazapertine is safe and well tolerated when administered orally. Analogs of mazapertine with conformational restriction have been prepared and have greater affinity for the 5-HT1A receptor.