ArticleAlcoholism, clinical and experimental research2018
Apremilast Alters Behavioral Responses to Ethanol in Mice: I. Reduced Consumption and Preference.
Article in Alcoholism, clinical and experimental research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 29 citations in OpenAlex.
- Global deletion ofbioRxiv : the preprint server for biology · 2026Article
- Repeated TLR7 activation induces cell type- and brain region-specific transcriptome changes in male mice.Scientific reports · 2026Article
- The effect of neuroimmune signalling on drug addiction.Frontiers in pharmacology · 2026Review
- Morphine and nicotine intake in high drinking in the dark mice is reduced by informatics-nominated and translationally relevant compounds.Frontiers in psychiatry · 2026Article
- Apremilast reduces co-occurring alcohol drinking and mechanical allodynia and regulates central amygdala GABAergic transmission.JCI insight · 2025Article
- Alcohol drinking is attenuated by PDE4 inhibition but partial microglia depletion is not sufficient to block stress-induced escalation of alcohol intake in female mice.Alcohol (Fayetteville, N.Y.) · 2025Article
- The PDE4 inhibitor apremilast modulates ethanol responses in Gabrb1-S409A knock-in mice via PKA-dependent and independent mechanisms.Neuropharmacology · 2024Article
- Targeting cAMP signaling and phosphodiesterase 4 for liver disease treatment.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2024Article
- Therapeutic perspectives on PDE4B inhibition in adipose tissue dysfunction and chronic liver injury.Expert opinion on therapeutic targets · 2024Review
- Inhibition of the Sodium-Calcium Exchanger Reverse Mode Activity Reduces Alcohol Consumption in Rats.International journal of molecular sciences · 2024Article
- Cell-type brain-region specific changes in prefrontal cortex of a mouse model of alcohol dependence.Neurobiology of disease · 2024Article
- Selective PDE4B and PDE4D inhibitors produce distinct behavioral responses to ethanol and GABAergic drugs in mice.Neuropharmacology · 2023Article
- Neuroinflammatory Response in Reward-Associated Psychostimulants and Opioids: A Review.Cellular and molecular neurobiology · 2023Review
- Neuroimmune pathways as targets to reduce alcohol consumption.Pharmacology, biochemistry, and behavior · 2023Article
- Apremilast-induced increases in acute ethanol intoxication and decreases in ethanol drinking in mice involve PKA phosphorylation of GABANeuropharmacology · 2022Article
- Targeting the Maladaptive Effects of Binge Drinking on Circadian Gene Expression.International journal of molecular sciences · 2022Article
- Immune treatments for alcohol use disorder: A translational framework.Brain, behavior, and immunity · 2021Review
- Deletion of Tlr3 reduces acute tolerance to alcohol and alcohol consumption in the intermittent access procedure in male mice.Addiction biology · 2021Article
- The Use of Apremilast in Psoriasis: An Indian Perspective on Real-World Scenarios.Psoriasis (Auckland, N.Z.) · 2021Review
- Immunological mechanisms and therapeutic targets of fatty liver diseases.Cellular & molecular immunology · 2021Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
backgroundPhosphodiesterase type 4 (PDE4) inhibitors produce widespread anti-inflammatory effects and reduce ethanol (EtOH) consumption in several rodent models. These drugs are potential treatments for several diseases, including central nervous system disorders, but clinical use is limited by their emetic activity. Apremilast is a selective PDE4 inhibitor with fewer gastrointestinal side effects that is FDA-approved for the treatment of psoriasis.
methodsWe measured the acute and chronic effects of apremilast on EtOH consumption in male and female C57BL/6J mice using the continuous and intermittent 24-hour 2-bottle choice drinking models. We also studied the effects of apremilast on preference for sucrose or saccharin, spontaneous locomotor activity, and blood EtOH clearance. Finally, apremilast levels in plasma, liver, and brain were measured 1 or 2 hours after injection.
resultsIn the continuous and intermittent drinking tests, apremilast (15 to 50 mg/kg, p.o.) dose dependently reduced EtOH intake and preference in male and female mice. Higher doses of apremilast (30 to 50 mg/kg) also reduced total fluid intake in these mice. Chronic administration of apremilast (20 mg/kg) produced a stable reduction in EtOH consumption in both drinking tests with no effect on total fluid intake. The drinking effects were reversible after drug treatment was replaced with vehicle administration (saline) for 2 to 4 days. Six daily apremilast injections did not alter preference for saccharin or sucrose in male or female mice. Apremilast (20 mg/kg) transiently decreased spontaneous locomotor activity and did not alter blood EtOH clearance. The highest levels of apremilast were found in liver followed by plasma and brain.
conclusionsApremilast produced stable reductions in voluntary EtOH consumption and was rapidly distributed to plasma and tissues (including the brain), suggesting that it may be an improved PDE4 inhibitor for medication development and repurposing efforts to treat alcohol abuse.
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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.