GPR139

2022-08-14: reference:

GPR139 #

• Antagonizes μ-Opioid Receptor
• The role of orphan receptor GPR139 in neuropsychiatric behavior
  • Mice with loss experiences schizophrenia-like symptomatology that is rescued with DAR antagonist haloperidol + naltrexone.
    • Indeed GPR139 has inhibitory actions on D2
  • loss of GPR139 in mice results in delayed onset hyperactivity and prominent neuropsychiatric manifestations including elevated stereotypy, increased anxiety-related traits, delayed acquisition of operant responsiveness, disruption of cued fear conditioning and social interaction deficits.

• Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia #