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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, but no trials beyond laboratory work in animals have been conducted to date.
- Characterization in rats of the anxiolytic potential of ELB139 [1-(4-chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-one], a new agonist at the benzodiazepine binding site of the GABAA receptor. Journal of Pharmacology and Experimental Therapeutics. 2005 Aug;314(2):717-24. PMID 15860576
- Atack JR. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opinion in Investigational Drugs. 2005 May;14(5):601-18. PMID 15926867
- Rabe H, Kronbach C, Rundfeldt C, Lüddens H. The novel anxiolytic ELB139 displays selectivity to recombinant GABA(A) receptors different from diazepam. Neuropharmacology. 2007 Mar;52(3):796-801. PMID 17087982
- Grunwald C, Rundfeldt C, Lankau HJ, Arnold T, Höfgen N, Dost R, Egerland U, Hofmann HJ, Unverferth K. Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. Journal of Medicinal Chemistry. 2006 Mar 23;49(6):1855-66. PMID 16539371
- Langen B, Rundfeldt C. 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 Behaviour. 2007 Jan;86(1):79-85. PMID 17257662
- Whiting PJ. GABA-A receptors: a viable target for novel anxiolytics? Current Opinion in Pharmacology. 2006 Feb;6(1):24-9. PMID 16359919
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