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Abecarnil
Systematic (IUPAC) name
propan-2-yl 4-(methoxymethyl)-6-(phenylmethoxy) -9H-pyrido[5,4-b]indole-3-carboxylate
Identifiers
CAS number 111841-85-1
ATC code none
PubChem 65914
ChemSpider 59323
Chemical data
Formula C 24H24N2O4  
Mol. mass 404.458 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life 3.4 hours (IV), 7 hours (oral)
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Abecarnil (ZK-112119) 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 GABAA receptors in the brain.[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 less problems of drug 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

References

  1. ^ Ozawa M, Nakada Y, Sugimachi K, Yabuuchi F, Akai T, Mizuta E, Kuno S, Yamaguchi M. Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates. Japanese Journal of Pharmacology. 1994 Mar;64(3):179-87.
  2. ^ Ozawa M, Nakada Y, Sugimachi K, et al. (March 1994). "Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates". Jpn. J. Pharmacol. 64 (3): 179–87. PMID 7912751. http://www.journalarchive.jst.go.jp/jnlpdf.php?cdjournal=jphs1951&cdvol=64&noissue=3&startpage=179&lang=en&from=jnlabstract.  
  3. ^ Aufdembrinke B. Abecarnil, a new beta-carboline, in the treatment of anxiety disorders. British Journal of Psychiatry 1998;(34):55-63.
  4. ^ Pinna G, Galici R, Schneider HH, Stephens DN, Turski L. Alprazolam dependence prevented by substituting with the beta-carboline abecarnil. Proceedings of the National Academy of Sciences U S A. 1997 Mar 18;94(6):2719-23.
  5. ^ Jung ME, Wallis CJ, Gatch MB, Lal H. Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal. Alcohol. 2000 Jun;21(2):161-8.
  6. ^ Löscher W, Hönack D (April 1992). "Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil". Naunyn Schmiedebergs Arch. Pharmacol. 345 (4): 452–60. PMID 1352384.  
  7. ^ Krause W, Schutt B, Duka T. Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man. Arzneimittelforschung. 1990 May;40(5):529-32.
  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. ^ Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH, Petersen EN, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. Journal of Pharmacology and Experimental Therapeutics. 1990 Apr;253(1):334-43.
  10. ^ Sannerud CA, Ator NA, Griffiths RR. Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence. Behavioural Pharmacology. 1992 Oct;3(5):507-516.
  11. ^ Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder. Psychopharmacology Bulletin. 1991;27(2):171-9.
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