Overview
- Peptide (C)DRRARFPSHEVEASR, corresponding to amino acid residues 239 - 253 of mouse GPR52 (Accession P0C5J4). 3rd intracellular loop.
- Mouse and rat brain lysates; human SH-SY5Y neuroblastoma cell lysate (1:200-1:1000).
Western blot analysis of mouse brain lysates (lanes 1 and 3) and rat brain lysates (lanes 2 and 4):1, 2. Anti-GPR52 Antibody (#AGR-058), (1:200).
3, 4. Anti-GPR52 Antibody, preincubated with GPR52 Blocking Peptide (#BLP-GR058) (#BLP-GR058).
- Rat brain sections (1:300).
G-Protein Coupled Receptor 52 (GPR52) is a conserved class-A orphan receptor, a member of the of the GPCR superfamily. The native ligand for GPR52 is unknown but the receptor has a high level of basal activity not related to ligand binding. Structure analysis shows that GPR52 extracellular loop 2 occupies the orthosteric binding pocket and operates as a built-in agonist, enabling an intrinsically high level of basal activity. The receptor also features a side pocket for ligand binding3.
Tissue distribution analysis of human, mouse, and rat indicates that GPR52 is expressed exclusively in the brain, especially in striatum. In the human brain, GPR52 expression profile overlaps with the distribution of D1 and D2 dopamine receptors which are associated with its function1.
GPR52 inhibits dopamine D2 receptor signaling and activates dopamine D1/NMDA receptors via intracellular cAMP accumulation2.
GPR52 is involved in the manifestation of schizophrenia, Huntington’s disease, cognitive impairment and hyperactivity and several other psychiatric disorders and hence it represents a promising therapeutic target. Agonists may potentially act as a novel class of antipsychotics1,2.
