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.[1][2]
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.[3] It has primarily anxiolytic and anticonvulsant effects, but produces little sedative effects or ataxia,[4] and has also been demonstrated in rats to increase serotonin levels in the striatum and prefrontal cortex, without affecting dopamine levels.[5] It has been proposed as a possible candidate for a novel non-sedating anxiolytic or anticonvulsant drug for use in humans[6] 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.[7] It was developed by Arzneimittelwerk Dresden in the 1990s.[8]
References
^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. PMID15860576. S2CID21967108.
^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:10.1517/13543784.14.5.601. PMID15926867. S2CID22793644.
^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. PMID17087982. S2CID21598180.
^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. PMID16539371.
^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. PMID17257662. S2CID22862432.
