| 词条 | Abecarnil |
| 释义 |
| Verifiedfields = changes | verifiedrevid = 477237117 | IUPAC_name = propan-2-yl 4-(methoxymethyl)-6-(phenylmethoxy) -9H-pyrido[5,4-b]indole-3-carboxylate | image = Abecarnil-2D-by-AHRLS-2012.png | tradename = | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = 3.4 hours (IV), 7 hours (oral) | excretion = | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 111841-85-1 | ATC_prefix = none | ATC_suffix = | PubChem = 65914 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 59323 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = IZM1PNJ3JL | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D02594 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 454095 | C=24 | H=24 | N=2 | O=4 | molecular_weight = 404.458 g/mol | smiles = COCc3c(C(=O)OC(C)C)ncc4[nH]c2ccc(OCc1ccccc1)cc2c34 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C24H24N2O4/c1-15(2)30-24(27)23-19(14-28-3)22-18-11-17(29-13-16-7-5-4-6-8-16)9-10-20(18)26-21(22)12-25-23/h4-12,15,26H,13-14H2,1-3H3 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = RLFKILXOLJVUNF-UHFFFAOYSA-N }}Abecarnil (ZK-112,119) is an anxiolytic drug from the β-Carboline family. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. It is a partial agonist acting selectively at the benzodiazepine site of the GABAA receptor.[1][2] Abecarnil was originally developed as an anti-anxiety drug, but has not as yet been commercially developed for use in humans, instead so far mainly being used for research into the development of other new sedative and anxiolytic drugs. Investigations are continuing into its actions and it looks likely to be developed for use both in the treatment of anxiety,[3] and as a less addictive substitute drug for the treatment of benzodiazepine[4] and alcohol[5] addiction. Abecarnil may also have fewer problems of tolerance and withdrawal problems compared to nonselective full agonist benzodiazepine acting drugs.[6] Abecarnil is a relatively subtype-selective drug which produces primarily anxiolytic effects, with comparatively less sedative or muscle relaxant properties,[7][8] and does not significantly potentiate the effects of alcohol.[9] The abuse potential of abecarnil is thought to be less than that of benzodiazepines,[10] with only mild withdrawal symptoms noted after abrupt discontinuation of treatment.[11] See also
References1. ^{{cite journal | last1 = Ozawa | first1 = M | last2 = Nakada | first2 = Y | last3 = Sugimachi | first3 = K | last4 = Yabuuchi | first4 = F | last5 = Akai | first5 = T | last6 = Mizuta | first6 = E | last7 = Kuno | first7 = S | last8 = Yamaguchi | first8 = M | date = Mar 1994 | title = Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates | url = | journal = Japanese Journal of Pharmacology | volume = 64 | issue = 3| pages = 179–87 | doi=10.1254/jjp.64.179 | pmid=7912751}} {{Anxiolytics}}{{GABAAR PAMs}}2. ^{{cite journal |vauthors=Ozawa M, Nakada Y, Sugimachi K |title=Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates |journal=Jpn. J. Pharmacol. |volume=64 |issue=3 |pages=179–87 |date=March 1994 |pmid=7912751 |doi= 10.1254/jjp.64.179|url=http://www.journalarchive.jst.go.jp/jnlpdf.php?cdjournal=jphs1951&cdvol=64&noissue=3&startpage=179&lang=en&from=jnlabstract|display-authors=etal}} 3. ^{{cite journal | author = Aufdembrinke B | year = 1998 | title = Abecarnil, a new beta-carboline, in the treatment of anxiety disorders | pmid =9829018 | journal = British Journal of Psychiatry | volume = 34 | issue = | pages = 55–63 }} 4. ^{{cite journal | doi = 10.1073/pnas.94.6.2719 |vauthors=Pinna G, Galici R, Schneider HH, Stephens DN, Turski L |date=Mar 1997 | title = Alprazolam dependence prevented by substituting with the beta-carboline abecarnil | url = | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 94 | issue = 6| pages = 2719–23 | pmc = 20156 }} 5. ^{{cite journal | doi = 10.1016/S0741-8329(00)00079-3 |vauthors=Jung ME, Wallis CJ, Gatch MB, Lal H |date=Jun 2000 | title = Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal | url = | journal = Alcohol | volume = 21 | issue = 2| pages = 161–8 | pmid = 10963939 }} 6. ^{{cite journal |vauthors=Löscher W, Hönack D |title=Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil |journal=Naunyn Schmiedebergs Arch. Pharmacol. |volume=345 |issue=4 |pages=452–60 |date=April 1992 |pmid=1352384 |doi= 10.1007/BF00176624|url=}} 7. ^{{cite journal |vauthors=Krause W, Schutt B, Duka T |date=May 1990 | title = Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man | url = | journal = Arzneimittelforschung | volume = 40 | issue = 5| pages = 529–32 | pmid = 1974428 }} 8. ^Duka T, Schutt B, Krause W, Dorow R, McDonald S, Fichte K. Human studies on abecarnil, a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. British Journal of Clinical Pharmacology. 1993 Apr;35(4):386-94. 9. ^{{cite journal |vauthors=Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH |date=Apr 1990 | title = Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors | url = | journal = Journal of Pharmacology and Experimental Therapeutics | volume = 253 | issue = 1| pages = 334–43 | pmid = 1970361 |display-authors=etal}} 10. ^{{cite journal |vauthors=Sannerud CA, Ator NA, Griffiths RR |date=Oct 1992 | title = Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence | url = | journal = Behavioural Pharmacology | volume = 3 | issue = 5| pages = 507–516 | pmid = 11224153 | doi=10.1097/00008877-199210000-00009}} 11. ^{{cite journal |vauthors=Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J | year = 1991 | title = The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder | url = | journal = Psychopharmacology Bulletin | volume = 27 | issue = 2| pages = 171–9 | pmid = 1681563 }} 7 : Anxiolytics|Beta-Carbolines|Phenol ethers|Ethers|Carboxylate esters|GABAA receptor positive allosteric modulators|Isopropyl esters |
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