Afobazole

Afobazole
Systematic (IUPAC) name
5-ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Clinical data
Pregnancy cat.  ?
Legal status ℞ Prescription only
Routes Oral
Identifiers
CAS number 173352-39-1
ATC code None
PubChem CID 9862937
ChemSpider 8038633 Y
UNII HDO6HX6NZU Y
Chemical data
Formula C15H21N3O2S 
Mol. mass 307.410 g/mol
SMILES eMolecules & PubChem
 Y(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, 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

  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". 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. 
GABAA PAMs
Abecarnil • Adipiplon • Alpidem • CGS-8216 • CGS-9896 • CGS-13767 • CGS-20625 • Divaplon • ELB-139 • Fasiplon • GBLD-345 • Gedocarnil • L-838,417 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • SL-651,498 • Taniplon • TP-003 • TP-13 • TPA-023 • Y-23684 • ZK-93423
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Afobazole • Opipramol
Others

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)
Receptor
Ligands
3-PPP • 4-IBP • 4-PPBP • Afobazole • Allylnormetazocine • Amitriptyline • Amphetamine • Berberine • Citalopram • Clorgyline • Cocaine • Cyclazocine • Dextrallorphan • Dextromethorphan • Dextrorphan • DTG • BD-1,008 • Desipramine • DHEA • Dimethyltryptamine • Dimemorfan • Ditolylguanidine • EMD-57,445 • Escitalopram • Fluoxetine • Fluvoxamine • Heroin • Igmesine • Imipramine • JO-1,784 • L-687,384 • Lamotrigine • Lu 28-179 • MDMA • Methamphetamine • Morphine • Noscapine • OPC-14,523 • Opipramol • PB-28 • PD-144,415 • Pentazocine • Pentoxyverine • Phencyclidine • PRE-084 • Pregnenolone • RTI-55 • SA-4503 • Sertraline • Siramesine • Venlafaxine
BD-1,047 • BD-1,063 • BMY-14,802 • E-5,842 • Haloperidol • NE-100 • Progesterone • Rimcazole • SM-21
Unknown