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Fabomotizole
Clinical data | |
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Trade names | Afobazole |
Other names | Obenoxazine |
Routes of administration |
Oral |
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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 |
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Chemical and physical data | |
Formula | C15H21N3O2S |
Molar mass | 307.41 g·mol−1 |
3D model (JSmol) | |
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NY (what is this?) (verify) |
Fabomotizole (INN; 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. 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. Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety.
Experiments of mice have shown antimutagenic and antiteratogenic properties.
Fabomotizole has found little clinical use outside Russia and has not been evaluated by the FDA.
See also
5-HT1AR agonists | |
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GABAAR PAMs |
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Gabapentinoids |
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Antidepressants |
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Sympatholytics |
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Others | |
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MT1 | |
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MT2 | |
Unsorted | |