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. PMID 15860576. S2CID 21967108.
^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. PMID 15926867. S2CID 22793644.
^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. PMID 17087982. S2CID 21598180.
^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. PMID 16539371.
^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. PMID 17257662. S2CID 22862432.
^Rogawski MA (June 2006). "Diverse mechanisms of antiepileptic drugs in the development pipeline". Epilepsy Research. 69 (3): 273–94. doi:10.1016/j.eplepsyres.2006.02.004. PMC1562526. PMID 16621450.
^Whiting PJ (February 2006). "GABA-A receptors: a viable target for novel anxiolytics?". Current Opinion in Pharmacology. 6 (1): 24–9. doi:10.1016/j.coph.2005.08.005. PMID 16359919.
^US 5869481, "Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making"
This article about an anxiolytic is a stub. You can help Wikipedia by expanding it.
anxiolytic, drug, with, novel, chemical, structure, which, used, scientific, research, similar, effects, benzodiazepine, drugs, structurally, distinct, classed, nonbenzodiazepine, anxiolytic, identifiersiupac, name, chlorophenyl, piperidin, dihydro, imidazol, . 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 139IdentifiersIUPAC name 1 4 Chlorophenyl 4 piperidin 1 yl 1 5 dihydro imidazol 2 oneCAS Number188116 08 7 YPubChem CID11277418ChemSpider9452418UNIIBKP2A5554FCompTox Dashboard EPA DTXSID40877536Chemical and physical dataFormulaC 14H 16Cl N 3OMolar mass277 75 g mol 13D model JSmol Interactive imageSMILES Clc3ccc cc3 N1CC NC1 O N2CCCCC2InChI InChI 1S C14H16ClN3O c15 11 4 6 12 7 5 11 18 10 13 16 14 18 19 17 8 2 1 3 9 17 h4 7H 1 3 8 10H2Key YGXIELIREXEJQN UHFFFAOYSA N verify ELB 139 is a subtype selective partial agonist at GABAA receptors with highest affinity for the a3 subtype but highest efficacy at a1 and a2 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 Edit Langen B Egerland U Bernoster 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 PMID 15860576 S2CID 21967108 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 PMID 15926867 S2CID 22793644 Rabe H Kronbach C Rundfeldt C Luddens 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 PMID 17087982 S2CID 21598180 Grunwald C Rundfeldt C Lankau HJ Arnold T Hofgen 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 PMID 16539371 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 PMID 17257662 S2CID 22862432 Rogawski MA June 2006 Diverse mechanisms of antiepileptic drugs in the development pipeline Epilepsy Research 69 3 273 94 doi 10 1016 j eplepsyres 2006 02 004 PMC 1562526 PMID 16621450 Whiting PJ February 2006 GABA A receptors a viable target for novel anxiolytics Current Opinion in Pharmacology 6 1 24 9 doi 10 1016 j coph 2005 08 005 PMID 16359919 US 5869481 Anticonvulsive 1 ar alk ylimidazolin 2 ones and process for making This article about an anxiolytic is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title ELB 139 amp oldid 1134692548, wikipedia, wiki, book, books, library,
