GPR139
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G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139 gene.[1][2] Research has shown that mice with loss of GCP139 experience schizophrenia-like symptomatology that is rescued with the dopamine receptor antagonist haloperidol and the μ-opioid receptor antagonist naltrexone.[3][4]
GPR139 is activated by L-tryptophan and L-phenylalanine, though only at relatively high concentrations,[5] but in 2025, GPR139 was identified as a novel opioid receptor, specifically of dynorphins.[6]
Ligands
[edit | edit source]Agonists
[edit | edit source]- JNJ-63533054
- Zelatriazin (TAK-41), (NBI-1065846) a potent, and GPR139 receptor selective agonist [7] which was in clinical trials to gauge the efficacy for treating psychiatric conditions such as major depressive disorder and the negative symptoms of schizophrenia, but was later dropped from development.
- TC-O 9311 [444932-31-4]
Antagonists
[edit | edit source]References
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Further reading
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