词条 | NS-2710 |
释义 |
| Watchedfields = changed | verifiedrevid = 424770500 | IUPAC_name = 1-[1-[3-(3-pyridyl)phenyl]benzimidazol-5-yl]ethanone O-ethyloxime | image = NS-2710.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 = | ATC_prefix = | ATC_suffix = | PubChem = 9863520 | DrugBank = | ChemSpiderID = 8039216 | C=22 | H=20 | N=4 | O=1 | molecular_weight = 356.420 g/mol | smiles = c4ncccc4-c(c2)cccc2-n3c1ccc(cc1nc3)C(C)=NOCC | StdInChI = 1S/C22H20N4O/c1-3-27-25-16(2)17-9-10-22-21(13-17)24-15-26(22)20-8-4-6-18(12-20)19-7-5-11-23-14-19/h4-15H,3H2,1-2H3/b25-16+ | StdInChIKey = NHJFEXZXSCFYRX-PCLIKHOPSA-N }}NS-2710 (LS-193,970) is an anxiolytic drug with a novel chemical structure, developed by the small pharmaceutical company NeuroSearch. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. NS-2710 is a potent but non-selective partial agonist at GABAA receptors, although with little efficacy at the α1 subtype and more at α2 and α3. It has anxiolytic effects comparable to chlordiazepoxide,[1] and while it is a less potent anticonvulsant than the related drug NS-2664, it has a much longer duration of action, and similarly to other α2/α3-preferring partial agonists produces little sedative effects or physical dependence.[2] References1. ^Evenden J, Duncan B, Ko T. A comparison of the effects of psychotomimetics and anxiolytics on punished and unpunished responding maintained by fixed interval schedules of food reinforcement in the rat. Behavioural Pharmacology. 2006 Feb;17(1):87-99. {{PMID|16377966}} {{Anxiolytics}}{{GABAAR PAMs}}{{nervous-system-drug-stub}}2. ^Mirza NR, Nielsen EØ. Do subtype-selective gamma-aminobutyric acid A receptor modulators have a reduced propensity to induce physical dependence in mice? Journal of Pharmacology and Experimental Therapeutics. 2006 Mar;316(3):1378-85. {{PMID|16352707}} 5 : Anxiolytics|Ketoximes|Benzimidazoles|Pyridines|GABAA receptor positive allosteric modulators |
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