In a previous post, the six major groups of antipsychotics were identified. Only a few months ago, in December of 2012, researchers in China identified and synthesized yet another antipsychotic derivative. This chemical group called Tetrahydroprotoberberine (THPB) derivatives have long been known to antagonize dopamine receptors. Now, they can be called a type of antipsychotic and be synthesized at a larger scale.
The researchers working at the at the Shanghai Institute of Materia Medica have found an efficient method that can be used to create an integral intermediate that is involved in the complete synthesis of THPBs. They eventually produced 31 specific THPB compounds, each containing different substituents on their carbon rings. All 31 were tested, resulting in the identification of compounds 18k and 18m as partial agonists of dopamine receptor D1, antagonists of D2, and agonists of serotonin receptor 5-HT(1A). These results suggest that the substances could reduce psychotic symptoms. When tested in animals, it was discovered that these two compounds do indeed work as antipsychotics. The researchers were able to conclude that if the two substances are targeted to different neurotransmitter receptors in the brains of people suffering from psychotic disorders, the symptoms of psychosis can be treated. Clearly, this research may lead to the development of drugs that can fight conditions of the brain in novel ways.
By Mariel Hohmann