2. Signaling Pathways
  3. GPCR/G Protein
  4. GPR52

GPR52

G Protein-Coupled Receptor 52

GPR52 is an orphan G-protein-coupled receptor that is selectively expressed in the striatum and cortex with the highest level of expression in the nucleus accumbens (NAc). The selective expression of GPR52 in the NAc and other striatal regions suggests an important function for this receptor in primary striatal neurons and broader corticostriatal circuitry. Moreover, GPR52 is colocalized exclusively with dopamine D2 receptors in medium spiny neurons (MSNs) in the striatum and has lesser expression in neurons of the medial prefrontal cortex. Notably in transgenic mice, the overexpression of GPR52 significantly decreased methamphetamine-induced locomotion, while GPR52 knockout mice showed an anxiolytic-like phenotype. Studies have indicated that GPR52 couples to Gas/olf- G proteins to activate adenylyl cyclase and modulate cAMP signaling and displays high levels of constitutive activity. Thus, GPR52 signaling via cAMP could oppose activity of D2 signaling in the striatum while stimulating the D1/N-methyl-d-aspartate (NMDA) function in the frontal cortex. Therefore, GPR52 may serve as a promising novel target for psychiatric disorders including schizophrenia and substance use disorders (SUDs).

GPR52 Related Products (5):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101787
    TP-024
    		99.96%
    TP-024 (FTBMT) is a selective GPR52 agonist with an EC50 of 75 nM. TP-024 has antipsychotic and procognitive properties.
    TP-024
  • HY-138639
    PW0787
    		99.18%
    PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior.
    PW0787
  • HY-145468
    GPR52 antagonist-1
    		98.92%
    GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons.
    GPR52 antagonist-1
  • HY-147395
    GPR52 agonist-1
    		99.76%
    GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.
    GPR52 agonist-1
  • HY-163671
    PW0729
    		Agonist
    PW0729 (compound 15b) is an orphan GPR52 agonist with potential applications in GPR52 activation, signaling bias, and neuropsychiatric and neurological disorders. The brain exposure characteristics of PW0729 need to be further optimized.
    PW0729