词条 | Fengabine |
释义 |
| IUPAC_name = (6Z)-6-[butylamino-(2-chlorophenyl)methylene]-4-chloro-cyclohexa-2,4-dien-1-one | image = Fengabine.png | tradename = | pregnancy_category = | legal_status = Uncontrolled | routes_of_administration = Oral | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 80018-06-0 | ATC_prefix = none | ATC_suffix = | PubChem = 5362066 | ChemSpiderID = 4514924 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = YQG0NJI5A7 | KEGG = D04149 | C=17 | H=17 | Cl=2 | N=1 | O=1 | molecular_weight = 322.23 g/mol }}Fengabine (SL-79,229) is a drug which was investigated as an antidepressant but was never marketed.[1][2] Its mechanism of action is unknown, but its antidepressant effects are reversed by GABAA receptor antagonists like bicuculline and it has hence been labeled as GABAergic; however, it does not actually bind to GABA receptors, nor does it inhibit GABA-T.[1][2] In clinical trials, fengabine's efficacy was comparable to that of the tricyclic antidepressants, but with a more rapid onset of action and much less side effects.[3][4][5] Notably, fengabine lacks any sedative effects.[4] See also
References1. ^1 {{cite journal | vauthors = Lloyd KG, Zivkovic B, Sanger D, Depoortere H, Bartholini G | title = Fengabine, a novel antidepressant GABAergic agent. I. Activity in models for antidepressant drugs and psychopharmacological profile | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 241 | issue = 1 | pages = 245–50 |date=April 1987 | pmid = 3033203 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3033203}} {{Antidepressants}}{{Anxiolytics}}2. ^1 {{cite journal | vauthors = Scatton B, Lloyd KG, Zivkovic B | title = Fengabine, a novel antidepressant GABAergic agent. II. Effect on cerebral noradrenergic, serotonergic and GABAergic transmission in the rat | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 241 | issue = 1 | pages = 251–7 |date=April 1987 | pmid = 3033204 | doi = | url = http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=3033204|display-authors=etal}} 3. ^{{cite journal | vauthors = Magni G, Garreau M, Orofiamma B, Palminteri R | title = Fengabine, a new GABAmimetic agent in the treatment of depressive disorders: an overview of six double-blind studies versus tricyclics | journal = Neuropsychobiology | volume = 20 | issue = 3 | pages = 126–31 | year = 1989 | pmid = 2668780 | doi = 10.1159/000118485| url = }} 4. ^1 {{cite journal | vauthors = Nielsen NP, Cesana B, Zizolfi S, Ascalone V, Priore P, Morselli PL | title = Therapeutic effects of fengabine, a new GABAergic agent, in depressed outpatients: a double-blind study versus clomipramine | journal = Acta Psychiatrica Scandinavica | volume = 82 | issue = 5 | pages = 366–71 |date=November 1990 | pmid = 2281807 | doi = 10.1111/j.1600-0447.1990.tb01402.x| url = }} 5. ^{{cite journal | vauthors = Fairweather DB, Kerr JS, Hilton S, Hindmarch I | title = A placebo controlled double-blind evaluation of the pharmacodynamics of fengabine vs amitriptyline following single and multiple doses in elderly volunteers | journal = British Journal of Clinical Pharmacology | volume = 35 | issue = 3 | pages = 278–83 |date=March 1993 | pmid = 8471403 | pmc = 1381575 | doi = 10.1111/j.1365-2125.1993.tb05695.x| url = }} 4 : Chloroarenes|Imines|Phenols|Drugs with unknown mechanisms of action |
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