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  3. Abecarnil - Wikipedia
Abecarnil - Wikipedia
From Wikipedia, the free encyclopedia

Abecarnil
Clinical data
Drug classGABAA receptor positive allosteric modulator; Anxiolytic
ATC code
  • None
Pharmacokinetic data
Elimination half-life3.4 hours (IV), 7 hours (oral)
Identifiers
  • propan-2-yl 4-(methoxymethyl)-6-(phenylmethoxy) -9H-pyrido[5,4-b]indole-3-carboxylate
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H24N2O4
Molar mass404.466 g·mol−1
3D model (JSmol)
  • COCc3c(C(=O)OC(C)C)ncc4[nH]c2ccc(OCc1ccccc1)cc2c34
  • InChI=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 checkY
  • Key:RLFKILXOLJVUNF-UHFFFAOYSA-N checkY
  (verify)

Abecarnil (developmental code name 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]

Development

Abecarnil was originally developed as an anti-anxiety drug, but has not as yet been commercially developed for use in humans. It has mainly been used for research into the development of other new sedative and anxiolytic drugs. Investigations are continuing into its actions, and it is likely to be developed for use in the treatment of anxiety[2] and as a less addictive substitute drug for the treatment of benzodiazepine[3] and alcohol[4] addiction.

Pharmacology

Abecarnil is a relatively subtype-selective drug that produces primarily anxiolytic effects, with comparatively fewer sedative or muscle relaxant properties.[5][6] Additionally, it does not significantly potentiate the effects of alcohol.[7]

Potential advantages

Abecarnil may have fewer problems with tolerance and withdrawal compared to nonselective full agonist benzodiazepine acting drugs.[8]

The abuse potential of abecarnil is thought to be less than that of benzodiazepines,[9] with only mild withdrawal symptoms noted after abrupt discontinuation of treatment.[10]

Photoswitchable analog

A photoswitchable analog of abecarnil (azocarnil) has been developed to locally and reversibly control neuroinhibition with light in wildtype animals.[11]

See also

References

  1. ^ Ozawa M, Nakada Y, Sugimachi K, Yabuuchi F, Akai T, Mizuta E, et al. (March 1994). "Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates". Japanese Journal of Pharmacology. 64 (3): 179–187. doi:10.1254/jjp.64.179. PMID 7912751.
  2. ^ Aufdembrinke B (1998). "Abecarnil, a new beta-carboline, in the treatment of anxiety disorders". The British Journal of Psychiatry. Supplement. 34 (34): 55–63. doi:10.1192/S0007125000293537. PMID 9829018. S2CID 24311570.
  3. ^ Pinna G, Galici R, Schneider HH, Stephens DN, Turski L (March 1997). "Alprazolam dependence prevented by substituting with the beta-carboline abecarnil". Proceedings of the National Academy of Sciences of the United States of America. 94 (6): 2719–2723. Bibcode:1997PNAS...94.2719P. doi:10.1073/pnas.94.6.2719. PMC 20156. PMID 9122263.
  4. ^ Jung ME, Wallis CJ, Gatch MB, Lal H (June 2000). "Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal". Alcohol. 21 (2): 161–168. doi:10.1016/S0741-8329(00)00079-3. PMID 10963939.
  5. ^ Krause W, Schütt B, Duka T (May 1990). "Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man". Arzneimittel-Forschung. 40 (5): 529–532. PMID 1974428.
  6. ^ Duka T, Schütt B, Krause W, Dorow R, McDonald S, Fichte K (April 1993). "Human studies on abecarnil a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile". British Journal of Clinical Pharmacology. 35 (4): 386–394. doi:10.1111/j.1365-2125.1993.tb04155.x. PMC 1381549. PMID 8097921.
  7. ^ Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, et al. (April 1990). "Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors". The Journal of Pharmacology and Experimental Therapeutics. 253 (1): 334–343. PMID 1970361.
  8. ^ 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-Schmiedeberg's Archives of Pharmacology. 345 (4): 452–460. doi:10.1007/BF00176624. PMID 1352384. S2CID 20486955.
  9. ^ Sannerud CA, Ator NA, Griffiths RR (October 1992). "Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence". Behavioural Pharmacology. 3 (5): 507–516. doi:10.1097/00008877-199210000-00009. PMID 11224153. S2CID 32081258.
  10. ^ Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, et al. (1991). "The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder". Psychopharmacology Bulletin. 27 (2): 171–179. PMID 1681563.
  11. ^ Maleeva G, Nin-Hill A, Wirth U, Rustler K, Ranucci M, Opar E, et al. (October 2024). "Light-Activated Agonist-Potentiator of GABAA Receptors for Reversible Neuroinhibition in Wildtype Mice". Journal of the American Chemical Society. doi:10.1021/jacs.4c08446. PMC 11503767. PMID 39383450.
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