Fabomotizole Explained

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. 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

• Mebicar
• Phenibut
• Selank
• Validol
• Bemethyl

Notes and References

1. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information. 2012. 26. 1. 63. 21 March 2015.
2. Neznamov GG, Siuniakov SA, Chumakov DV, Bochkarev VK, Seredenin SB . [Clinical study of the selective anxiolytic agent afobazol] . Eksperimental'naia i Klinicheskaia Farmakologiia . 64 . 2 . 15–19 . 2001 . 11548440 .
3. Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS . [Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon] . Eksperimental'naia i Klinicheskaia Farmakologiia . 68 . 1 . 20–24 . 2005 . 15786959 .
4. Seredin SB, Melkumian DS, Val'dman EA, Iarkova MA, Seredina TC, Voronin MV, Lapitskaia AS . [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 . 16878488 .
5. Antipova TA, Sapozhnikova DS, Bakhtina LI, Seredenin SB . [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 . 19334503 .
6. Seredenin SB, Antipova TA, Voronin MV, Kurchashova SY, Kuimov AN . Interaction of afobazole with sigma1-receptors . Bulletin of Experimental Biology and Medicine . 148 . 1 . 42–44 . July 2009 . 19902093 . 10.1007/s10517-009-0624-x . 37411324 .
7. Medvedev VE, Trosnova AP, Dobrovol'skiĭ AV . [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 . 18379478 .
8. Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB . [Antimutagenic and antiteratogenic properties of afobazole] . Eksperimental'naia i Klinicheskaia Farmakologiia . 72 . 1 . 46–51 . Jan–Feb 2009 . 19334511 .
9. Katnik C, Garcia A, Behensky AA, Yasny IE, Shuster AM, Seredenin SB, Petrov AV, Seifu S, McAleer J, Willing A, Cuevas J . Treatment with afobazole at delayed time points following ischemic stroke improves long-term functional and histological outcomes . Neurobiol Dis . 62 . 354-364 . February 2014 . 24141021. 10.1016/j.nbd.2013.10.011 .