ArticleFrontiers in pain research (Lausanne, Switzerland)2021
GPR171 Agonist Reduces Chronic Neuropathic and Inflammatory Pain in Male, But Not Female Mice.
Article in Frontiers in pain research (Lausanne, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 17 citations in OpenAlex.
- Targeting GCell reports. Medicine · 2026Article
- No evidence of immediate or persistent analgesic effect from a single dose of psilocybin in three mouse models of pain.Nature communications · 2026Article
- Zingerone alleviates acute seizures by reducing intrinsic hippocampal neuronal excitability in a rat model of temporal lobe epilepsy.Frontiers in neuroscience · 2026Article
- Surgical Pleth Index as a Potentially Useful and Noninvasive Tool for Assessing Tracheal Intubation Conditions in Female Patients During Neuromuscular Blockade-Free Anesthesia.Emergency medicine international · 2026Article
- Comprehensive analysis of circRNA-miRNA-mRNA networks to reveal potential cell death, inflammation and oxidative stress-related targets for postoperative cognitive dysfunction.Frontiers in aging neuroscience · 2026Article
- Psilocybin has no immediate or persistent analgesic effect in acute and chronic mouse pain models.bioRxiv : the preprint server for biology · 2025Article
- ProSAAS neuropeptides and receptors GPR171 and GPR83: Potential therapeutic applications for pain, anxiety, and body weight regulation.The Journal of pharmacology and experimental therapeutics · 2025Review
- Zingerone alleviates inflammatory pain by reducing the intrinsic excitability of anterior cingulate cortex neurons in a mice model.Frontiers in pharmacology · 2025Article
- GPCRs: emerging targets for novel T cell immune checkpoint therapy.Cancer immunology, immunotherapy : CII · 2024Review
- The role of orphan G protein-coupled receptors in pain.Heliyon · 2024Review
- A small molecule ligand for the novel pain target, GPR171, produces minimal reward in mice.Pharmacology, biochemistry, and behavior · 2023Article
- Gpr83 Tunes Nociceptor Function, Controlling Pain.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2023Article
- Cellular and circuit diversity determines the impact of endogenous opioids in the descending pain modulatory pathway.Frontiers in systems neuroscience · 2022Review
- DNA Methylation: A Target in Neuropathic Pain.Frontiers in medicine · 2022Review
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
Chronic pain is a growing public health crisis that requires exigent and efficacious therapeutics. GPR171 is a promising therapeutic target that is widely expressed through the brain, including within the descending pain modulatory regions. Here, we explore the therapeutic potential of the GPR171 agonist, MS15203, in its ability to alleviate chronic pain in male and female mice using a once-daily systemic dose (10 mg/kg, i.p.) of MS15203 over the course of 5 days. We found that in our models of Complete Freund's Adjuvant (CFA)-induced inflammatory pain and chemotherapy-induced peripheral neuropathy (CIPN), MS15203 did not alleviate thermal hypersensitivity and allodynia, respectively, in female mice. On the other hand, MS15203 treatment decreased the duration of thermal hypersensitivity in CFA-treated male mice following 3 days of once-daily administration. MS15203 treatment also produced an improvement in allodynia in male mice, but not female mice, in neuropathic pain after 5 days of treatment. Gene expression of GPR171 and that of its endogenous ligand BigLEN, encoded by the gene PCSK1N, were unaltered within the periaqueductal gray (PAG) in both male and female mice following inflammatory and neuropathic pain. However, following neuropathic pain in male mice, the protein levels of GPR171 were decreased in the PAG. Treatment with MS15203 then rescued the protein levels of GPR171 in the PAG of these mice. Taken together, our results identify GPR171 as a GPCR that displays sexual dimorphism in alleviation of chronic pain. Further, our results suggest that GPR171 and MS15203 have demonstrable therapeutic potential in the treatment of chronic pain.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.