Fabomotizole

Last updated

Fabomotizole
Fabomotizole.svg
Fabomotizol.png
Clinical data
Trade names Afobazole
Other namesObenoxazine
Routes of
administration 		Oral
Legal status
Legal status
  • US:UnscheduledNot FDA approved
Pharmacokinetic data
Bioavailability 43.64%, pronounced first-pass effect
Metabolism extensive hepatic
Onset of action 0.85±0.13 hours
Elimination half-life 0.82±0.54 hours
Identifiers
  • 4-[2-[(6-ethoxy-1H-benzimidazol-2-yl)sulfanyl]ethyl]morpholine
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C15H21N3O2S
Molar mass 307.41 g·mol−1
3D model (JSmol)
  • CCOc3ccc2nc(SCCN1CCOCC1)[nH]c2c3
  • InChI=1S/C15H21N3O2S/c1-2-20-12-3-4-13-14(11-12)17-15(16-13)21-10-7-18-5-8-19-9-6-18/h3-4,11H,2,5-10H2,1H3,(H,16,17) Yes check.svgY
  • Key:WWNUCVSRRUDYPP-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)
Afobazole from Russia Afobazole.jpg
Afobazole from Russia

Fabomotizole (INN; [1] brand name Afobazole) is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions.[ citation needed ] Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. [2] [3] [4] [5] [6] Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety. [7]

Experiments in mice have shown antimutagenic and antiteratogenic properties. [8]

Experiments in rats have shown beneficial effect in the model of ischemic stroke. [9]

Fabomotizole has found little clinical use outside Russia and has not been evaluated by the FDA.

See also

References

  1. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. 26 (1): 63. 2012. Retrieved 21 March 2015.
  2. ↑ Neznamov GG, Siuniakov SA, Chumakov DV, Bochkarev VK, Seredenin SB (2001). "[Clinical study of the selective anxiolytic agent afobazol]". Eksperimental'naia i Klinicheskaia Farmakologiia. 64 (2): 15–19. PMID   11548440.
  3. ↑ Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS (2005). "[Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon]". Eksperimental'naia i Klinicheskaia Farmakologiia. 68 (1): 20–24. PMID   15786959.
  4. ↑ Seredin SB, Melkumian DS, Val'dman EA, Iarkova MA, Seredina TC, Voronin MV, Lapitskaia AS (2006). "[Effects of afobazole on the BDNF content in brain structures of inbred mice with different phenotypes of emotional stress reaction]". Eksperimental'naia i Klinicheskaia Farmakologiia. 69 (3): 3–6. PMID   16878488.
  5. ↑ Antipova TA, Sapozhnikova DS, Bakhtina LI, Seredenin SB (2009). "[Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons]". Eksperimental'naia i Klinicheskaia Farmakologiia. 72 (1): 12–14. PMID   19334503.
  6. ↑ Seredenin SB, Antipova TA, Voronin MV, Kurchashova SY, Kuimov AN (July 2009). "Interaction of afobazole with sigma1-receptors". Bulletin of Experimental Biology and Medicine. 148 (1): 42–44. doi:10.1007/s10517-009-0624-x. PMID   19902093. S2CID   37411324.
  7. ↑ Medvedev VE, Trosnova AP, Dobrovol'skiĭ AV (2007). "[Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole]". Zhurnal Nevrologii I Psikhiatrii imeni S.S. Korsakova. 107 (7): 25–29. PMID   18379478.
  8. ↑ Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB (Jan–Feb 2009). "[Antimutagenic and antiteratogenic properties of afobazole]". Eksperimental'naia i Klinicheskaia Farmakologiia. 72 (1): 46–51. PMID   19334511.
  9. ↑ Katnik C, Garcia A, Behensky AA, Yasny IE, Shuster AM, Seredenin SB, Petrov AV, Seifu S, McAleer J, Willing A, Cuevas J (February 2014). "Treatment with afobazole at delayed time points following ischemic stroke improves long-term functional and histological outcomes". Neurobiol Dis. 62: 354–364. doi:10.1016/j.nbd.2013.10.011. PMID   24141021.
This page is based on this Wikipedia article
Text is available under the CC BY-SA 4.0 license; additional terms may apply.
Images, videos and audio are available under their respective licenses.