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Open Access Articles- Top Results for Fabomotizole

Fabomotizole

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Fabomotizole
200px
Systematic (IUPAC) name
5-Ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Clinical data
Trade names Afobazole
  • US: Not approved
Oral
Pharmacokinetic data
Metabolism extensive hepatic
Half-life 0,82±0,54 h
Identifiers
173352-39-1 7pxN
N05BX04
PubChem CID 9862937
ChemSpider 8038633 7pxY
UNII HDO6HX6NZU 7pxY
Synonyms Fabomotizole
Chemical data
Formula C15H21N3O2S
307.410 g/mol
 14pxN (what is this?)  (verify)

Fabomotizole[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 antagonism, 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]

Fabomotizole has found little clinical use outside of Russia and has not been evaluated by the FDA.

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. PMID 19902093. doi:10.1007/s10517-009-0624-x. 
  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. 

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