Afobazol

Afobazol
(IUPAC) ime
5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Klinički podaci
Identifikatori
CAS broj 173352-39-1
ATC kod nije dodeljen
PubChem[1][2] 9862937
ChemSpider[3] 8038633
Hemijski podaci
Formula C15H21N3O2S 
Mol. masa 307.410 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status ℞ Prescription only
Način primene Oralno

Afobazol je lek sa anksiolitičkim i neurozaštitnim dejstvom. On ne deluje kao sedativ ili relaksant mišića, te je stoga njegovo dejstvo selektivnije od mnogih drugih lekova sa sličnom primenom. Ovaj lek se pojavio na ruskom tržištu ranih 2000-tih.

Mehanizam dejstva afobazola je delimično poznat. Smatra se da promoviše oslobađanje GABA, NGF i BDNF, da je antagonist MT1 i MT3 receptor, kao i agonist sigma receptora.[4][5][6][7][8]

Klinička ispitivanja su pokazala da je afobazol dobro tolerisan i da je efikasan u lečenju anksioznosti. Šira klinička ispitivanja izvan Rusije još nisu izvršena.[9]

Literatura

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ 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. 
  5. ↑ 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. 
  6. ↑ 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. 
  7. ↑ 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. 
  8. ↑ 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. 
  9. ↑ Medvedev, VE; Trosnova, AP; Dobrovol'skiĭ, AV (2007). „Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole”. Zhurnal nevrologii i psikhiatrii imeni S.S. Korsakova / Ministerstvo zdravookhraneniia i meditsinskoi promyshlennosti Rossiiskoi Federatsii, Vserossiiskoe obshchestvo nevrologov [i] Vserossiiskoe obshchestvo psikhiatrov 107 (7): 25–9. PMID 18379478.