Fabomotizole

Fabomotizole
Clinical data
Trade names Afobazole
Routes of
administration		 Oral
ATC code N05BX04 (WHO)
Legal status
Legal status
  • US: Not FDA approved; unscheduled
Pharmacokinetic data
Bioavailability 43.64%, pronounced first-pass effect
Metabolism extensive hepatic
Onset of action 0.85±0.13 hours
Biological half-life 0.82±0,54 hours
Identifiers
Synonyms Fabomotizole
CAS Number 173352-39-1 N
PubChem (CID) 9862937
ChemSpider 8038633 YesY
UNII HDO6HX6NZU YesY
Chemical and physical data
Formula C15H21N3O2S
Molar mass 307.410 g/mol
3D model (Jmol) Interactive image
 NYesY (what is this?)  (verify)
Afobazole from Russia

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 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

  1. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information. 26 (1): 63. 2012. Retrieved 21 March 2015.
  2. ↑ Neznamov, GG; Siuniakov, SA; Chumakov, DV; Bochkarev, VK; Seredenin, SB (2001). "Clinical study of the selective anxiolytic agent afobazol". Eksperimental'naia i klinicheskaia farmakologiia. 64 (2): 15–9. PMID 11548440.
  3. ↑ Silkina, IV; Gan'shina, TC; Seredin, SB; Mirzoian, RS (2005). "Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon". Eksperimental'naia i klinicheskaia farmakologiia. 68 (1): 20–4. PMID 15786959.
  4. ↑ Seredin, SB; Melkumian, DS; Val'dman, EA; Iarkova, MA; Seredina, TC; Voronin, MV; Lapitskaia, AS (2006). "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. PMID 16878488.
  5. ↑ Antipova, TA; Sapozhnikova, DS; Bakhtina, LIu; Seredenin, SB (2009). "Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons". Eksperimental'naia i klinicheskaia farmakologiia. 72 (1): 12–4. PMID 19334503.
  6. ↑ Seredenin, SB; Antipova, TA; Voronin, MV; Kurchashova, SY; Kuimov, AN (2009). "Interaction of afobazole with sigma1-receptors". Bulletin of experimental biology and medicine. 148 (1): 42–4. doi:10.1007/s10517-009-0624-x. PMID 19902093.
  7. ↑ Medvedev, VE; Trosnova, AP; Dobrovol'skiĭ, AV (2007). "Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole". Zh Nevrol Psikhiatr Im S S Korsakova. 107 (7): 25–9. PMID 18379478.
  8. ↑ Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB (Jan–Feb 2009). "Antimutagenic and antiteratogenic properties of afobazole". Eksp Klin Farmakol. 72 (1): 46–51. PMID 19334511.


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