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G protein-coupled receptor 88 (GPR88)
- Target
- GPR88
- Molecular classification
- G protein-coupled receptor, GPCR, Class A/rhodopsin-like orphan GPCR
01
Overview
GPR88 is an orphan G protein-coupled receptor (GPCR) highly expressed in the striatum. It couples to Gi/o proteins, inhibiting adenylyl cyclase activity. GPR88 modulates other GPCRs, such as opioid receptors, and is implicated in neuropsychiatric disorders like ADHD, schizophrenia and bipolar disorder. While the endogenous ligand remains unknown, synthetic agonists have been developed. It is a promising drug target for neuropsychiatric disorders due to its role in modulating striatal function and impulsivity-related behaviors.
- Other names
- STRGStriatum-specific G-protein coupled receptor
02
Mechanism of action
Allosteric modulation via binding to a cytoplasmic pocket formed by transmembrane segments 5/6 and part of the α5 helix of Gi1 protein.
03
Biological functions
Signal transductionInhibition of adenylyl cyclase activityModulation of other GPCR signalingGi/o protein coupling
04
Disease associations
Attention Deficit/Hyperactivity Disorder (ADHD)SchizophreniaBipolar disorderSpeech delayChorea
05
Interacting drugs
(1R,2R)-2-PCCA
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