{"id":"eltanolone","rwe":[{"pmid":"33483729","year":"2021","title":"Structure-Activity Relationship of Neuroactive Steroids, Midazolam, and Perampanel Toward Mitigating Tetramine-Triggered Activity in Murine Hippocampal Neuronal Networks.","finding":"","journal":"Toxicological sciences : an official journal of the Society of Toxicology","studyType":"Clinical Study"},{"pmid":"28428226","year":"2017","title":"Rapid Throughput Analysis of GABA(A) Receptor Subtype Modulators and Blockers Using DiSBAC(1)(3) Membrane Potential Red Dye.","finding":"","journal":"Molecular pharmacology","studyType":"Clinical Study"},{"pmid":"22826603","year":"2012","title":"Comparative molecular field analysis to derive pharmacophore maps for disposition parameters of intravenous anaesthetic agents.","finding":"","journal":"British journal of anaesthesia","studyType":"Clinical Study"},{"pmid":"21205625","year":"2011","title":"Comparative molecular field analysis to derive pharmacophore maps for induction doses of intravenous anaesthetic agents.","finding":"","journal":"British journal of anaesthesia","studyType":"Clinical Study"},{"pmid":"20430765","year":"2010","title":"Development of pharmacophoric maps for cardiovascular depression by intravenous anaesthetic agents: comparison with maps for immobilizing activity.","finding":"","journal":"British journal of anaesthesia","studyType":"Clinical Study"}],"tags":[{"label":"eltanolone","category":"class"},{"label":"Small Molecule","category":"modality"},{"label":"GABA-A receptor alpha-1/beta-2/gamma-2","category":"target"},{"label":"GABRA1","category":"gene"},{"label":"GABRB2","category":"gene"},{"label":"GABRG2","category":"gene"},{"label":"Active","category":"status"},{"label":"Anesthetics","category":"pharmacology"},{"label":"Central Nervous System Agents","category":"pharmacology"},{"label":"Central Nervous System Depressants","category":"pharmacology"}],"phase":"phase_2","safety":{},"trials":[],"aliases":[],"patents":[],"pricing":[],"allNames":"pregnanolone","offLabel":[],"synonyms":["eltanolone","pregnanolone"],"timeline":[],"aiSummary":"Eltanolone, also known as pregnanolone, is a small molecule drug that targets the GABA-A receptor alpha-1/beta-2/gamma-2 subunits. It is a potent anesthetic agent that works by enhancing the inhibitory effects of GABA, a neurotransmitter that helps to calm down neuronal activity. Eltanolone is not FDA-approved for any indications, and its commercial status is unknown. As a potent anesthetic, it requires careful consideration of its potential side effects, including respiratory depression and sedation. Further research is needed to fully understand its safety and efficacy profile.","approvals":[],"brandName":"Pregnanolone","ecosystem":[],"mechanism":{"target":"GABA-A receptor alpha-1/beta-2/gamma-2, GABA-A receptor; anion channel","targets":[{"gene":"GABRA1","source":"DrugCentral","target":"GABA-A receptor alpha-1/beta-2/gamma-2","protein":"Gamma-aminobutyric acid receptor subunit alpha-1"},{"gene":"GABRB2","source":"DrugCentral","target":"GABA-A receptor alpha-1/beta-2/gamma-2","protein":"Gamma-aminobutyric acid receptor subunit beta-2"},{"gene":"GABRG2","source":"DrugCentral","target":"GABA-A receptor alpha-1/beta-2/gamma-2","protein":"Gamma-aminobutyric acid receptor subunit gamma-2"}],"modality":"Small Molecule","drugClass":"eltanolone","explanation":"Imagine your brain is like a busy city, with lots of different signals and activities happening all the time. GABA is like a traffic cop that helps to slow down the traffic and keep things calm. Eltanolone is like a special tool that helps the traffic cop do its job even better, by making it easier for GABA to calm down the activity in the brain.","oneSentence":"Eltanolone works by enhancing the activity of GABA, a neurotransmitter that helps to calm down neuronal activity.","technicalDetail":"Eltanolone is a positive allosteric modulator of the GABA-A receptor, specifically targeting the alpha-1/beta-2/gamma-2 subunits. This enhances the receptor's affinity for GABA, leading to increased chloride ion influx and hyperpolarization of the neuronal membrane, resulting in sedative and anesthetic effects."},"commercial":{},"references":[{"id":1,"url":"https://drugcentral.org/drugcard/997","fields":["approvals","synonyms","ATC","PK","indications","contraindications","DDIs","targets","patents","FAERS"],"source":"DrugCentral"},{"id":2,"url":"https://clinicaltrials.gov/search?intr=ELTANOLONE","fields":["trials"],"source":"ClinicalTrials.gov"},{"id":3,"url":"https://pubmed.ncbi.nlm.nih.gov/?term=ELTANOLONE","fields":["publications"],"source":"PubMed/NCBI"}],"_enrichedAt":"2026-03-30T10:58:18.222485","biosimilars":[],"competitors":[{"drugName":"alprazolam","drugSlug":"alprazolam","fdaApproval":"1981-10-16","genericCount":24,"patentStatus":"Off-patent — generic 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