Afobazole

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Afobazole
File:Afobazole structure.png
Systematic (IUPAC) name
5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 173352-39-1
ATC code none
PubChem CID 9862937
Chemical data
Formula C15H21N3O2S
Molar mass 307.410 g/mol[[Script error: No such module "String".]]
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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, 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, MT1 receptor antagonism, MT3 receptor antagonism, and sigma agonism 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

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  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