Chemistry:Fabomotizole
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| Trade names | Afobazole |
| Other names | Obenoxazine |
| Routes of administration | Oral |
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| 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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| Formula | C15H21N3O2S |
| Molar mass | 307.41 g·mol−1 |
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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 of mice have shown antimutagenic and antiteratogenic properties.[8]
Fabomotizole has found little clinical use outside Russia and has not been evaluated by the FDA.
See also
References
- ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN)". WHO Drug Information 26 (1): 63. 2012. https://www.who.int/medicines/publications/druginformation/issues/RL67.pdf. Retrieved 21 March 2015.
- ↑ "[Clinical study of the selective anxiolytic agent afobazol]". Eksperimental'naia i Klinicheskaia Farmakologiia 64 (2): 15–19. 2001. PMID 11548440.
- ↑ "[Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon]". Eksperimental'naia i Klinicheskaia Farmakologiia 68 (1): 20–24. 2005. PMID 15786959.
- ↑ "[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. 2006. PMID 16878488.
- ↑ "[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. 2009. PMID 19334503.
- ↑ "Interaction of afobazole with sigma1-receptors". Bulletin of Experimental Biology and Medicine 148 (1): 42–44. July 2009. doi:10.1007/s10517-009-0624-x. PMID 19902093.
- ↑ "[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. 2007. PMID 18379478.
- ↑ "[Antimutagenic and antiteratogenic properties of afobazole]". Eksperimental'naia i Klinicheskaia Farmakologiia 72 (1): 46–51. Jan–Feb 2009. PMID 19334511.
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