G protein-coupled receptor 171 (GPR171)

G protein-coupled receptor 171 (GPR171) is a class A, rhodopsin-like, seven-transmembrane G protein-coupled receptor that was initially classified as an orphan receptor but has since been identified as the receptor for the neuropeptide BigLEN, a product of proSAAS cleavage[1][2][3][4]. GPR171 is enriched in the brain, notably in the basolateral amygdala and periaqueductal gray, and participates in the regulation of feeding behavior, body weight, anxiety, pain (through modulation of opioid signaling), and immune responses (particularly negative regulation of T cells)[1][2][3][8]. It is considered a therapeutic target for obesity, pain, and certain neuropsychiatric conditions, as well as cancer where its expression is associated with altered cell differentiation and migration[1][2][3][4]. The receptor is activated by endogenous BigLEN and can be targeted by selective small molecule agonists and antagonists[3][4].

Other names

GPR171G-protein coupled receptor H963H963Platelet activating receptor homologF730001G15RikProbable G-protein coupled receptor 171Platelet activating factor H963

Agonists and antagonists modulate feeding behavior and pain perception via G(i)-alpha signaling Inhibits myeloid differentiation and modulates opioid receptor pathways Alters metabolic and neurobehavioral pathways through neuropeptide-dependent activation