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Afobazole
Systematic (IUPAC) name
5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Identifiers
CAS number  ?
ATC code  ?
PubChem 9862937
Chemical data
Formula C 15H21N3O2S 
Mol. mass 307.410 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status investigational new drug
Routes  ?

Afobazole is an anxiolytic drug developed in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions, making it more selective in action than many currently used drugs for this application. Its mechanism of action remains poorly defined however, with GABAergic, NGF and BDNF release promoting, and sigma agonist actions all thought to have some involvement.[1][2][3][4][5] Clinical trials have shown afobazole to be well tolerated and reasonably effective for the treatment of anxiety, although it has yet to be introduced into widespread clinical use outside of Russia.[6]

References

  1. ^ Neznamov GG, Siuniakov SA, Chumakov DV, Bochkarev VK, Seredenin SB. Clinical study of the selective anxiolytic agent afobazol. Eksp Klin Farmakol. 2001 Mar-Apr;64(2):15-9. Russian. PMID 11548440
  2. ^ Silkina IV, Gan'shina TC, Seredin SB, Mirzoian RS. Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon. Eksp Klin Farmakol. 2005 Jan-Feb;68(1):20-4. Russian. PMID 15786959
  3. ^ 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. Eksp Klin Farmakol. 2006 May-Jun;69(3):3-6. Russian. PMID 16878488
  4. ^ Antipova TA, Sapozhnikova DS, Bakhtina LIu, Seredenin SB. Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons. Eksp Klin Farmakol. 2009 Jan-Feb;72(1):12-4. Russian. PMID 19334503
  5. ^ Seredenin SB, Antipova TA, Voronin MV, Kurchashova SY, Kuimov AN. Interaction of Afobazole with sigma(1)-Receptors. Bull Exp Biol Med. 2009 Jul;148(1):42-4. English, Russian. PMID 19902093
  6. ^ Medvedev VE, Trosnova AP, Dobrovol'skiĭ AV. Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole. Zh Nevrol Psikhiatr Im S S Korsakova. 2007;107(7):25-9. Russian. PMID 18379478
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