ELB-139 explained

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 GABA_A 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 registered a clinical trial in ClinicalTrials.govfor 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

1. Langen B, Egerland U, Bernöster K, Dost R, Unverferth K, Rundfeldt C . 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 . August 2005 . 15860576 . 10.1124/jpet.105.084681 . 21967108 .
2. Atack JR . 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 . May 2005 . 15926867 . 10.1517/13543784.14.5.601 . 22793644 .
3. Rabe H, Kronbach C, Rundfeldt C, Lüddens H . 21598180 . The novel anxiolytic ELB139 displays selectivity to recombinant GABA(A) receptors different from diazepam . Neuropharmacology . 52 . 3 . 796–801 . March 2007 . 17087982 . 10.1016/j.neuropharm.2006.09.013 .
4. Grunwald C, Rundfeldt C, Lankau HJ, Arnold T, Höfgen N, Dost R, Egerland U, Hofmann HJ, Unverferth K . 6 . Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors . Journal of Medicinal Chemistry . 49 . 6 . 1855–66 . March 2006 . 16539371 . 10.1021/jm0509400 .
5. Langen B, Rundfeldt C . 22862432 . 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 . January 2007 . 17257662 . 10.1016/j.pbb.2006.12.010 .
6. Rogawski MA . Diverse mechanisms of antiepileptic drugs in the development pipeline . Epilepsy Research . 69 . 3 . 273–94 . June 2006 . 16621450 . 1562526 . 10.1016/j.eplepsyres.2006.02.004 .
7. Whiting PJ . GABA-A receptors: a viable target for novel anxiolytics? . Current Opinion in Pharmacology . 6 . 1 . 24–9 . February 2006 . 16359919 . 10.1016/j.coph.2005.08.005 .
8. US . 5869481 . Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making .