ELB-139

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IUPAC_name = 1-(4-Chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-one


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PubChem = 11277418
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C=14|H=16|Cl=1|N=3|O=1
molecular_weight = 277.749 g/mol
smiles = Clc3ccc(cc3)N1CC(=NC1=O)N2CCCCC2
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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. [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]

ELB-139 is a subtype-selective partial agonist at GABA_A receptors, with highest affinity for the α3 subtype, but highest efficacy at α1 and α2. [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] It has primarily anxiolytic and anticonvulsant effects, but produces little sedative effects or ataxia, [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] and has also been demonstrated in rats to increase serotonin levels in the striatum and prefrontal cortex, without affecting dopamine levels. [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] 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. [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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