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Int. J. Mol. Sci. 2015, 16(6), 14109-14121;

Novel Therapeutic GPCRs for Psychiatric Disorders

Novartis Pharma, Medical Division, CNS Medical Franchise Department, Tokyo 105-6333, Japan
Received: 28 March 2015 / Revised: 25 May 2015 / Accepted: 9 June 2015 / Published: 19 June 2015
(This article belongs to the Collection G Protein-Coupled Receptor Signaling and Regulation)
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G protein-coupled receptors (GPCRs) are the most common targets of the neuropharmacological drugs in the central nervous system (CNS). GPCRs are activated by manifold neurotransmitters, and their activation in turn evokes slow synaptic transmission. They are deeply involved in multiple neurological and psychiatric disorders such as Parkinson’s disease and schizophrenia. In the brain, the striatum is strongly innervated by the ventral tegmental area (VTA) and plays a central role in manifestation of psychiatric disorders. Recently, anatomical and comprehensive transcriptome analysis of the non-odorant GPCR superfamily revealed that the orphan GPCRs GPR88, GPR6, and GPR52, as well as dopamine D1 and D2 receptors and the adenosine A2a receptor, are the most highly enriched in the rodent striatum. Genetically engineered animal models and molecular biological studies have suggested that these striatally enriched GPCRs have a potential to be therapeutic psychiatric receptors. This review summarizes the current understanding of the therapeutic GPCR candidates for psychiatric disorders. View Full-Text
Keywords: psychiatric disorders; striatum; schizophrenia; GPCR; GPR52; dopamine receptors; GPR88; GPR6 psychiatric disorders; striatum; schizophrenia; GPCR; GPR52; dopamine receptors; GPR88; GPR6

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Komatsu, H. Novel Therapeutic GPCRs for Psychiatric Disorders. Int. J. Mol. Sci. 2015, 16, 14109-14121.

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