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G-protein coupled receptor 139 (GPR139)

Target: GPR139
Molecular classification: G protein-coupled receptor, GPCR, Rhodopsin-like GPCR

Overview

G-protein coupled receptor 139 is an orphan rhodopsin-family GPCR highly expressed in specific brain regions. It primarily signals via (G_{q/11}), may respond to aromatic amino acids or peptide hormones endogenously—and represents an emerging target for neuropsychiatric drug development due to its restricted CNS distribution and behavioral effects observed upon genetic deletion.

Other names: GPRg1PGR3

Mechanism of action

GPR139 agonists; Dopamine D2 receptor antagonists; μ-opioid receptor antagonists

Biological functions

Signal transductionMood regulationReward processing

Disease associations

SchizophreniaDepressionNeuropsychiatric disorders

Interacting drugs

Zelatriazin (TAK‐41; NBI‐1065846)

2 more in the full profile.

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