ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2018
Preclinical evaluation of the kappa-opioid receptor antagonist CERC-501 as a candidate therapeutic for alcohol use disorders.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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44 citing papers in PubMed, 75 citations in OpenAlex.
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- Synchrony between midbrain gene transcription and dopamine terminal regulation is modulated by chronic alcohol drinking.Nature communications · 2025Article
- Epigenetic Dysregulation in Alcohol-Associated Behaviors: Preclinical and Clinical Evidence.Current topics in behavioral neurosciences · 2025Review
- Functional interaction between orexin/dynorphin transmission in the posterior paraventricular nucleus of the thalamus following alcohol dependence: mediation of alcohol-seeking behavior.Frontiers in pharmacology · 2025Article
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- Novel medications for problematic alcohol use.The Journal of clinical investigation · 2024Review
- LY2444296, a κ-opioid receptor antagonist, selectively reduces alcohol drinking in male and female Wistar rats with a history of alcohol dependence.Scientific reports · 2024Article
- Different mechanisms underlie compulsive alcohol self-administration in male and female rats.Biology of sex differences · 2024Article
- Sex differences in ethanol consumption and drinking despite negative consequences following adolescent social isolation stress in male and female rats.Physiology & behavior · 2023Article
- Activation of GABANeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- Systemic kappa opioid receptor antagonism accelerates reinforcement learning via augmentation of novelty processing in male mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- An epigenetic mechanism for over-consolidation of fear memories.Molecular psychiatry · 2022Article
- Article
- Dynorphin/Kappa Opioid Receptor Activity Within the Extended Amygdala Contributes to Stress-Enhanced Alcohol Drinking in Mice.Biological psychiatry · 2022Article
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9 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Prior work suggests a role of kappa-opioid signaling in the control of alcohol drinking, in particular when drinking is escalated due to alcohol-induced long-term neuroadaptations. Here, we examined the small molecule selective kappa antagonist CERC-501 in rat models of alcohol-related behaviors, with the objective to evaluate its potential as a candidate therapeutic for alcohol use disorders. We first tested the effect of CERC-501 on acute alcohol withdrawal-induced anxiety-like behavior. CERC-501 was then tested on basal as well as escalated alcohol self-administration induced by 20% alcohol intermittent access. Finally, we determined the effects of CERC-501 on relapse to alcohol seeking triggered by both stress and alcohol-associated cues. Control experiments were performed to confirm the specificity of CERC-501 effects on alcohol-related behaviors. CERC-501 reversed anxiety-like behavior induced by alcohol withdrawal. It did not affect basal alcohol self-administration but did dose-dependently suppress self-administration that had escalated following long-term intermittent access to alcohol. CERC-501 blocked relapse to alcohol seeking induced by stress, but not when relapse-like behavior was triggered by alcohol-associated cues. The effects of CERC-501 were observed in the absence of sedative side effects and were not due to effects on alcohol metabolism. Thus, in a broad battery of preclinical alcohol models, CERC-501 has an activity profile characteristic of anti-stress compounds. Combined with its demonstrated preclinical and clinical safety profile, these data support clinical development of CERC-501 for alcohol use disorders, in particular for patients with negatively reinforced, stress-driven alcohol seeking and use.
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