Enhancement of 5-HT2A receptor function and blockade of Kv1.5 by MK801 and ketamine: implications for PCP derivative-induced disease models

Abstract

Serotonin: Flipping a cellular switch The drugs ketamine and MK801, which are derivatives of phencyclidine (PCP, or angel dust), may provide clues to treatment of schizophrenia and hypertension. Both ketamine and MK801 have been reported to induce symptoms of schizophrenia and hypertension, and are used as to study these illnesses. The two drugs are known to affect serotonin receptors, but the mechanism remains unclear. Young Min Bae at Konkuk University School of Medicine, Chungju, South Korea, and colleagues investigated how ketamine and MK801 interact with a type of electrically activated biological switch known as a voltage-gated ion channel to influence serotonin receptors. They found that both ketamine and MK801 blocked the switch and enhanced activity of serotonin receptors, with MK801 having a stronger effect than ketamine. These results may help identify drug targets for treating hypertension and schizophrenia.