ArticleAlcoholism, clinical and experimental research2022
Effect of a brain-penetrant selective estrogen receptor degrader (SERD) on binge drinking in female mice.
Article in Alcoholism, clinical and experimental research, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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8 citing papers in PubMed, 10 citations in OpenAlex.
- Associations of plasma sex-related hormone and protein levels and alcohol dependence.Addiction (Abingdon, England) · 2025Article
- Adolescent Alcohol Exposure Dysregulates Developing Cortical GABA Circuits.Advances in experimental medicine and biology · 2025Review
- Rapid nongenomic estrogen signaling controls alcohol drinking behavior in mice.Nature communications · 2024Article
- Heart rate variability: A primer for alcohol researchers.Alcohol (Fayetteville, N.Y.) · 2024Article
- Sex- and estrous-related response patterns for alcohol depend critically on the level of compulsion-like challenge.Progress in neuro-psychopharmacology & biological psychiatry · 2024Article
- Fetal Cannabinoid Syndrome: Behavioral and Brain Alterations of the Offspring Exposed to Dronabinol during Gestation and Lactation.International journal of molecular sciences · 2024Article
- Sex differences in heart rate variability measures that predict alcohol drinking in rats.Addiction biology · 2024Article
- Effect of a brain-penetrant selective estrogen receptor degrader (SERD) on binge drinking in female mice.Alcoholism, clinical and experimental research · 2022Article
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9 authors at 2 institutions in 1 country.
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Abstract
backgroundGreater circulating levels of the steroid hormone 17β-estradiol (E2) are associated with higher levels of binge drinking in women. In female mice, estrogen receptors in the ventral tegmental area, a dopaminergic region of the brain involved in the motivation to consume ethanol, regulate binge-like ethanol intake. We recently developed a brain-penetrant selective estrogen receptor degrader (SERD), YL3-122, that could be used to test the behavioral role of brain estrogen receptors. We hypothesized that treating female mice with this compound would reduce binge-like ethanol drinking.
methodsFemale C57BL/6J mice were treated systemically with YL3-122 and a related SERD with low brain penetrance, XR5-27, and tested for binge-like ethanol consumption in the drinking in the dark (DID) test. Mice were also tested for sucrose and water consumption and blood ethanol clearance after treatment with the SERDs. Finally, the effect of ethanol exposure on Esr1 gene expression was measured in the ventral tegmental area (VTA), prefrontal cortex (PFC), and ventral hippocampus (vHPC) of male and female mice by quantitative real-time PCR after 4 DID sessions.
resultsYL3-122 reduced ethanol consumption when mice were in diestrus but not estrus. YL3-122 also decreased sucrose consumption but did not alter water intake or blood ethanol clearance. XR5-27 did not affect any of these measures. Binge-like ethanol drinking resulted in increased Esr1 transcript in the VTA of both sexes, male vHPC, and female PFC.
conclusionsThese results indicate that SERD treatment can decrease binge-like ethanol drinking in female mice. Thus, it could be a novel strategy to reduce binge drinking in women, with the caveat that effectiveness may depend on menstrual cycle phase. In addition, Esr1 transcript is increased by binge ethanol exposure in both sexes but in a brain region-specific manner.
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