Fabomotizole

Anxiolytic drug From Wikipedia, the free encyclopedia

Fabomotizole

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]

Quick Facts Clinical data, Trade names ...
Fabomotizole
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Clinical data
Trade namesAfobazole
Other namesObenoxazine
Routes of
administration
Oral
Legal status
Legal status
  • US: Unscheduled Not FDA approved
Pharmacokinetic data
Bioavailability43.64%, pronounced first-pass effect
Metabolismextensive hepatic
Onset of action0.85±0.13 hours
Elimination half-life0.82±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
FormulaC15H21N3O2S
Molar mass307.41 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) Y
  • Key:WWNUCVSRRUDYPP-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)
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Afobazole from Russia

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

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