Multiple Central Nervous System G protein-coupled receptors (CNS GPCRs)

Multiple Central Nervous System (CNS) G protein-coupled receptors (GPCRs) represent a vast class of integral membrane proteins that facilitate signal transduction across neuronal and glial cells (Hauser et al., Nature Reviews Drug Discovery, 2018). These receptors, including dopamine, serotonin, glutamate, and GABA-B receptors, are the primary mediators of neurotransmission and are essential for maintaining homeostasis in the brain (IUPHAR/BPS Guide to Pharmacology). In the context of drug development, the term often refers to the polypharmacological profile of neuropsychiatric medications that bind to a variety of these receptors to exert their clinical effects (Journal of Clinical Psychiatry, 2017). For instance, atypical antipsychotics like clozapine and olanzapine achieve their efficacy by modulating a specific subset of dopamine and serotonin receptors, which helps alleviate symptoms of psychosis (StatPearls, Antipsychotic Medications). However, the broad expression of these receptors throughout the CNS and peripheral tissues also leads to significant side effects, such as metabolic disturbances and sedation. Understanding the collective interaction of a drug with multiple CNS GPCRs is crucial for optimizing therapeutic outcomes in complex neurological and psychiatric disorders.

Other names

CNS GPCRsCentral Nervous System G protein-coupled receptorsMulti-target CNS receptorsNeurotransmitter GPCRs

Simultaneous modulation (antagonism, agonism, or partial agonism) of various neurotransmitter receptors including dopamine, serotonin, adrenergic, muscarinic, and histamine receptors to achieve therapeutic effects while balancing side profiles.