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Researchers Learn How a Brain Receptor is Activated
The discovery could potentially improve treatments for anxiety and depression

The National Institute of Mental Health (NIMH) on June 20, 2023, released highlights from a study it funded indicating that researchers have identified a molecule that binds to the GPR158 receptor and triggers its activity. In other words, they’ve discovered what activates brain receptors.

Metabotropic receptors are locations on the surface of nerve cells, or neurons, that help cells communicate with each other. When signaling molecules bind to them, these receptors are activated.

The study reported, “GPR158 is a G protein-coupled receptor highly expressed in the brain, especially in the prefrontal cortex, which is responsible for thought, planning, and emotion and is linked to mental disorders. However, GPR158 is not well understood, and a molecule that activates it had not been identified—until now. The findings highlight the importance of GPR158 as a receptor capable of altering activity in an area of the brain important for understanding and treating mental disorders. This discovery presents a potential new target for developing improved treatments for mental disorders like anxiety and depression.”

Experts noted that the study is significant and matters greatly because it reveals several new findings including:

  • “Glycine is the first (and only) transmitter for GPR158, which did not have an identified signaling molecule until now.
  • GPR158 is the first G protein-coupled receptor for glycine, which had previously been shown to bind only to ion channels.
  • Glycine has an excitatory effect on the G protein-coupled receptor, which contrasts its inhibitory effect on ion channels.”

The findings will prove important for understanding and treating mental disorders and for improving treatments for mental disorders such as anxiety and depression.