Afobazole ▪ Sale
Afobazole
Afobazole.svg
Systematic (IUPAC) name
5-Ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Clinical data
Legal status
  • US: Not approved
Routes Oral
Pharmacokinetic data
Half-life 0.4 hours
Identifiers
CAS number 173352-39-1
ATC code None
PubChem CID 9862937
ChemSpider 8038633
UNII HDO6HX6NZU
Chemical data
Formula C15H21N3O2S
Mol. mass 307.410 g/mol
 AfobazoleN (what is this?)  (verify)

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. Afobazole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. Clinical trials have shown afobazole to be well tolerated and reasonably effective for the treatment of anxiety.

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

References

  1. 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. 
  2. 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. 
  3. 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. 
  4. 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. 
  5. 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. 
  6. 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. 
Source of information: Wikipedia, the free encyclopedia - Disclaimer.

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