| 词条 | ELB-139 |
| 释义 |
| verifiedrevid = 451925233 | IUPAC_name = 1-(4-Chlorophenyl)-4-piperidin-1-yl-1,5-dihydro-imidazol-2-one | image = ELB-139.png | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 188116-08-7 | ATC_prefix = | ATC_suffix = | PubChem = 11277418 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID = 9452418 | C=14 | H=16 | Cl=1 | N=3 | O=1 | molecular_weight = 277.749 g/mol | smiles = Clc3ccc(cc3)N1CC(=NC1=O)N2CCCCC2 | StdInChI = 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,1-3,8-10H2 | StdInChIKey = YGXIELIREXEJQN-UHFFFAOYSA-N }}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] References1. ^{{cite journal | last1 = Langen | first1 = B | last2 = Egerland | first2 = U | last3 = Bernöster | first3 = K | last4 = Dost | first4 = R | last5 = Unverferth | first5 = K | last6 = Rundfeldt | first6 = C | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 314 | issue = 2 | pages = 717–24 | year = 2005 | pmid = 15860576 | doi = 10.1124/jpet.105.084681 }} {{Anxiolytics}}{{GABAAR PAMs}}{{nervous-system-drug-stub}}2. ^{{cite journal | last1 = Atack | first1 = JR | title = The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics | journal = Expert Opinion on Investigational Drugs | volume = 14 | issue = 5 | pages = 601–18 | year = 2005 | pmid = 15926867 | doi = 10.1517/13543784.14.5.601 }} 3. ^{{cite journal | last1 = Rabe | first1 = H | last2 = Kronbach | first2 = C | last3 = Rundfeldt | first3 = C | last4 = Lüddens | first4 = H | title = The novel anxiolytic ELB139 displays selectivity to recombinant GABA(A) receptors different from diazepam | journal = Neuropharmacology | volume = 52 | issue = 3 | pages = 796–801 | year = 2007 | pmid = 17087982 | doi = 10.1016/j.neuropharm.2006.09.013 }} 4. ^{{cite journal | last1 = Grunwald | first1 = C | last2 = Rundfeldt | first2 = C | last3 = Lankau | first3 = HJ | last4 = Arnold | first4 = T | last5 = Höfgen | first5 = N | last6 = Dost | first6 = R | last7 = Egerland | first7 = U | last8 = Hofmann | first8 = HJ | last9 = Unverferth | first9 = K | title = Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors | journal = Journal of Medicinal Chemistry | volume = 49 | issue = 6 | pages = 1855–66 | year = 2006 | pmid = 16539371 | doi = 10.1021/jm0509400 }} 5. ^{{cite journal | last1 = Langen | first1 = B | last2 = Rundfeldt | first2 = C | title = ELB139 an agonist at the benzodiazepine binding site increases 5-HT in the striatum and prefrontal cortex of rats: a microdialysis study | journal = Pharmacology Biochemistry and Behavior | volume = 86 | issue = 1 | pages = 79–85 | year = 2007 | pmid = 17257662 | doi = 10.1016/j.pbb.2006.12.010 }} 6. ^{{cite journal | last1 = Rogawski | first1 =MA | title = Diverse mechanisms of antiepileptic drugs in the development pipeline | journal = Epilepsy Res | volume = 69 | issue = 3 | pages = 273–294 | year = 2006 | pmid = 16621450 | doi=10.1016/j.eplepsyres.2006.02.004 | pmc=1562526}} 7. ^{{cite journal | last1 = Whiting | first1 = PJ | title = GABA-A receptors: a viable target for novel anxiolytics? | journal = Current Opinion in Pharmacology | volume = 6 | issue = 1 | pages = 24–9 | year = 2006 | pmid = 16359919 | doi = 10.1016/j.coph.2005.08.005 }} 8. ^US Patent 5869481 Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making 7 : Anxiolytics|Chloroarenes|Imidazolines|Ureas|Lactams|Piperidines|GABAA receptor positive allosteric modulators |
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