Wednesday, May 22, 2019

Functional Selective D2 Ligands for the Treatment of Schizophrenia-Novel Approaches in Drug Designing & Development-JuniperPublishers

JUNIPER PUBLISHERS-Novel Approaches in Drug Designing & Development


Functional Selective D2 Ligands for the Treatment of Schizophrenia


Authored by Xin Chen*

Functionally selective ligands (also known as biased ligands) of dopamine D2 receptors have been considered as not only valuable tools for dissecting the roles of D2-mediated G protein-dependent and independent signaling pathways, but also better antipsychotic drug candidates for neurological and psychiatric disorders including schizophrenia. Consequently, functionally selective D2R ligands have also been increasingly pursued by the biomedical community as promising antipsychotic therapeutics with improved efficacy and reduced side effects compared with unbiased ligands. This review will discuss the recent development in the discovery of functional selective D2R ligands. Schizophrenia is a chronic and severe mental disorder characterized by abnormal social behavior and failure to understand reality. Clinically, the disorder manifests with a large variety of symptoms that fall into three categories: positive, negative, and cognitive. Schizophrenia affects about 1.1% of world wide population. Although schizophrenia is not as common as other mental disorders such as anxiety disorder (18.1%), depression (6.9%), and bipolar disorder (2.6%), the symptoms can be very disabling. Therefore, it is often associated with high levels of morbidity and mortality. The average life expectancy of people with schizophrenia is ten to twenty-five years less than for the general population. This is the result of increased physical health problems and a higher suicide rate (about 10%)

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