Chemistry:ELB-139
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| Formula | C14H16ClN3O |
| Molar mass | 277.75 g·mol−1 |
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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.[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
- ↑ "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. doi:10.1124/jpet.105.084681. PMID 15860576.
- ↑ "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. doi:10.1517/13543784.14.5.601. PMID 15926867.
- ↑ "The novel anxiolytic ELB139 displays selectivity to recombinant GABA(A) receptors different from diazepam". Neuropharmacology 52 (3): 796–801. March 2007. doi:10.1016/j.neuropharm.2006.09.013. PMID 17087982.
- ↑ "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. doi:10.1021/jm0509400. PMID 16539371.
- ↑ "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. doi:10.1016/j.pbb.2006.12.010. PMID 17257662.
- ↑ "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research 69 (3): 273–94. June 2006. doi:10.1016/j.eplepsyres.2006.02.004. PMID 16621450.
- ↑ "GABA-A receptors: a viable target for novel anxiolytics?". Current Opinion in Pharmacology 6 (1): 24–9. February 2006. doi:10.1016/j.coph.2005.08.005. PMID 16359919.
- ↑ "Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making" US patent 5869481
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