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

GPR52 (G蛋白偶联受体52)

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 相关产品 (2):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101787
    TP-024 99.96%
    TP-024 (FTBMT) 是选择性的 GPR52 激动剂, EC50 为 75 nM。TP-024 有抗精神病和促进认知活性。
  • HY-138639
    PW0787 99.18%
    PW0787 是一种有效的,选择性的,具有口服活性的,可透过血脑屏障的 GPR52 激动剂 (EC50=135 nM)。PW0787 抑制精神刺激行为。