Fabomotizole

Fabomotizole

Systematic (IUPAC) name
5-Ethoxy-2-[2-(morpholino)-ethylthio]benzimidazole
Clinical data
Trade names	Afobazole
Routes of administration	Oral
Legal status
Legal status	US: Unscheduled
Pharmacokinetic data
Bioavailability	43.64%, pronounced first-pass effect
Metabolism	extensive hepatic
Onset of action	0.85±0.13 hours
Biological half-life	0.82±0,54 hours
Identifiers
CAS Number	173352-39-1
ATC code	N05BX04 (WHO)
PubChem	CID 9862937
ChemSpider	8038633
UNII	HDO6HX6NZU
Synonyms	Fabomotizole
Chemical data
Formula	C15H21N3O2S
Molar mass	307.410 g/mol
SMILES C3COCCN3CCSc(nc1c2)nc1ccc2OCC
InChI InChI=1S/C15H21N3O2S/c1-2-20-12-3-4-13-14(11-12)17-15(16-13)21-10-7-18-5-8-19-9-6-18/h3-4,11H,2,5-10H2,1H3,(H,16,17) Key:WWNUCVSRRUDYPP-UHFFFAOYSA-N
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Fabomotizole (INN)^[1] (brand name 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 agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors.^{[2][3][4][5][6]} Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety.^[7]

Experiments of mice have shown antimutagenic and antiteratogenic properties.^[8]

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

See also

• Mebicar
• Phenibut
• Selank
• Tenoten
• Validol

References

1. "International Nonproprietary Names for Pharmaceutical Substances (INN)" (PDF). WHO Drug Information 26 (1): 63. 2012. Retrieved 21 March 2015.
2. 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.
3. 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.
4. 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.
5. 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.
6. 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.
7. 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.
8. Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB. (Jan–Feb 2009). "Antimutagenic and antiteratogenic properties of afobazole". Eksp Klin Farmakol 72 (1): 46–51. PMID 19334511.