ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2013
A novel brain penetrant NPS receptor antagonist, NCGC00185684, blocks alcohol-induced ERK-phosphorylation in the central amygdala and decreases operant alcohol self-administration in rats.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers, 1 of them a synthesis that pooled it.
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Who cites it
21 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.
- Neuropeptide S modulation of learning and memory: a systematic review.Behavioral and brain functions : BBF · 2026Pooled it
- Neuropeptide S Protects Dopaminergic Neurons in a Paraquat-Induced Parkinson's Model Using SH-SY5Y Cells.Molecular neurobiology · 2026Article
- A Role for Neuropeptide S in Alcohol and Cocaine Seeking.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Role of the Neuropeptide S System in Emotionality, Stress Responsiveness and Addiction-Like Behaviours in Rodents: Relevance to Stress-Related Disorders.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Pharmacology, Physiology and Genetics of the Neuropeptide S System.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Pharmacological profile of the neuropeptide S receptor: Dynamic mass redistribution studies.Pharmacology research & perspectives · 2018Article
- Genome-Wide Expression Profiles Drive Discovery of Novel Compounds that Reduce Binge Drinking in Mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Article
- Critical Role for GFrontiers in psychiatry · 2018Article
- Neuropeptide systems and new treatments for nicotine addiction.Psychopharmacology · 2017Review
- The melanin-concentrating hormone-1 receptor modulates alcohol-induced reward and DARPP-32 phosphorylation.Psychopharmacology · 2016Article
- Homer2 regulates alcohol and stress cross-sensitization.Addiction biology · 2016Article
- Human Neuropeptide S Receptor Is Activated via a Gαq Protein-biased Signaling Cascade by a Human Neuropeptide S Analog Lacking the C-terminal 10 Residues.The Journal of biological chemistry · 2016Article
- Molecular Mechanism: ERK Signaling, Drug Addiction, and Behavioral Effects.Progress in molecular biology and translational science · 2016Review
- Emerging targets for addiction neuropharmacology: From mechanisms to therapeutics.Progress in brain research · 2016Review
- Ethanol activates midkine and anaplastic lymphoma kinase signaling in neuroblastoma cells and in the brain.Journal of neurochemistry · 2015Article
- Article
- Elabela-apelin receptor signaling pathway is functional in mammalian systems.Scientific reports · 2015Article
- Identification of neuropeptide S antagonists: structure-activity relationship studies, X-ray crystallography, and in vivo evaluation.ACS chemical neuroscience · 2014Article
- Neuronal extracellular signal-regulated kinase (ERK) activity as marker and mediator of alcohol and opioid dependence.Frontiers in integrative neuroscience · 2014Review
- Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.Journal of medicinal chemistry · 2013Article
Corrections and comments
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Authors and funding
17 authors at 4 institutions in 3 countries.
Funding
Abstract
The Neuropeptide S receptor, a Gs/Gq-coupled GPCR expressed in brain regions involved in mediating drug reward, has recently emerged as a candidate therapeutic target in addictive disorders. Here, we describe the in vitro and in vivo pharmacology of a novel, selective and brain penetrant NPSR antagonist with nanomolar affinity for the NPSR, NCGC00185684. In vitro, NCGC00185684 shows biased antagonist properties, and preferentially blocks ERK-phosphorylation over intracellular cAMP or calcium responses to NPS. In vivo, systemic NCGC00185684 blocks alcohol-induced ERK-phosphorylation in the rat central amygdala, a region involved in regulation of alcohol intake. NCGC00185684 also decreases operant alcohol self-administration, and lowers motivation for alcohol reward as measured using progressive ratio responding. These effects are behaviorally specific, in that they are observed at doses that do not influence locomotor activity or reinstatement responding following extinction. Together, these data provide an initial validation of the NPSR as a therapeutic target in alcoholism.
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Registered trials
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.