|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||277.75 g·mol−1|
|3D model (JSmol)|
ELB-139 (LS-191,811) is an anxiolytic drug with a novel chemical structure, which is used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.
ELB-139 is a subtype-selective partial agonist at GABAA receptors, with highest affinity for the α3 subtype, but highest efficacy at α1 and α2. It has primarily anxiolytic and anticonvulsant effects, but produces little sedative effects or ataxia, and has also been demonstrated in rats to increase serotonin levels in the striatum and prefrontal cortex, without affecting dopamine levels. It has been proposed as a possible candidate for a novel non-sedating anxiolytic or anticonvulsant drug for use in humans The sponsor elbion AG registered a clinical trial in ClinicalTrials.gov for the treatment of anxiety associated with panic disorder but the results have not been reported. It was developed by Arzneimittelwerk Dresden in the 1990s.
- Langen B, Egerland U, Bernöster K, Dost R, Unverferth K, Rundfeldt C (August 2005). "Characterization in rats of the anxiolytic potential of ELB139 [1-(4-chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-on], a new agonist at the benzodiazepine binding site of the GABAA receptor". The Journal of Pharmacology and Experimental Therapeutics. 314 (2): 717–24. doi:10.1124/jpet.105.084681. PMID 15860576.
- Atack JR (May 2005). "The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics". Expert Opinion on Investigational Drugs. 14 (5): 601–18. doi:10.1517/135437188.8.131.521. PMID 15926867.
- Rabe H, Kronbach C, Rundfeldt C, Lüddens H (March 2007). "The novel anxiolytic ELB139 displays selectivity to recombinant GABA(A) receptors different from diazepam". Neuropharmacology. 52 (3): 796–801. doi:10.1016/j.neuropharm.2006.09.013. PMID 17087982. S2CID 21598180.
- Grunwald C, Rundfeldt C, Lankau HJ, Arnold T, Höfgen N, Dost R, et al. (March 2006). "Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors". Journal of Medicinal Chemistry. 49 (6): 1855–66. doi:10.1021/jm0509400. PMID 16539371.
- Langen B, Rundfeldt C (January 2007). "ELB139 an agonist at the benzodiazepine binding site increases 5-HT in the striatum and prefrontal cortex of rats: a microdialysis study". Pharmacology, Biochemistry, and Behavior. 86 (1): 79–85. doi:10.1016/j.pbb.2006.12.010. PMID 17257662. S2CID 22862432.
- Rogawski MA (June 2006). "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research. 69 (3): 273–94. doi:10.1016/j.eplepsyres.2006.02.004. PMC 1562526. PMID 16621450.
- Whiting PJ (February 2006). "GABA-A receptors: a viable target for novel anxiolytics?". Current Opinion in Pharmacology. 6 (1): 24–9. doi:10.1016/j.coph.2005.08.005. PMID 16359919.
- US 5869481, "Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making"
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