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]
Clinical data | |
---|---|
Trade names | Afobazole |
Other names | Obenoxazine |
Routes of administration | Oral |
Legal status | |
Legal status |
|
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 | |
| |
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) | |
| |
| |
(what is this?) (verify) |
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
Wikiwand in your browser!
Seamless Wikipedia browsing. On steroids.
Every time you click a link to Wikipedia, Wiktionary or Wikiquote in your browser's search results, it will show the modern Wikiwand interface.
Wikiwand extension is a five stars, simple, with minimum permission required to keep your browsing private, safe and transparent.