Fabomotizole

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.^{[citation needed]} 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]

Fabomotizole

Clinical data
Trade names	Afobazole
Other names	Obenoxazine
Routes of administration	Oral
Legal status
Legal status	US: Unscheduled Not FDA approved
Pharmacokinetic data
Bioavailability	43.64%, pronounced first-pass effect
Metabolism	extensive hepatic
Onset of action	0.85±0.13 hours
Elimination half-life	0.82±0.54 hours
Identifiers
IUPAC name 4-[2-[(6-ethoxy-1H-benzimidazol-2-yl)sulfanyl]ethyl]morpholine
CAS Number	173352-21-1
PubChem CID	9862937
DrugBank	DB13623
ChemSpider	8038633
UNII	0F8K1X115C
KEGG	D10561
ChEBI	CHEBI:135309
ChEMBL	ChEMBL3707307
CompTox Dashboard (EPA)	DTXSID00169606
Chemical and physical data
Formula	C15H21N3O2S
Molar mass	307.41 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCOc3ccc2nc(SCCN1CCOCC1)[nH]c2c3
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) Y Key:WWNUCVSRRUDYPP-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Afobazole from Russia

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

Experiments in rats have shown beneficial effect in the model of ischemic stroke.^[9]

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

See also

• Mebicar
• Phenibut
• Selank
• Validol
• Bemethyl
• List of Russian drugs

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): 15–19. 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): 20–24. 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 LI, 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): 12–14. PMID 19334503.
6. Seredenin SB, Antipova TA, Voronin MV, Kurchashova SY, Kuimov AN (July 2009). "Interaction of afobazole with sigma1-receptors". Bulletin of Experimental Biology and Medicine. 148 (1): 42–44. doi:10.1007/s10517-009-0624-x. PMID 19902093. S2CID 37411324.
7. 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. 107 (7): 25–29. PMID 18379478.
8. Durnev AD, Zhanataev AK, Shreder OV, Seredenin SB (Jan–Feb 2009). "[Antimutagenic and antiteratogenic properties of afobazole]". Eksperimental'naia i Klinicheskaia Farmakologiia. 72 (1): 46–51. PMID 19334511.
9. Katnik C, Garcia A, Behensky AA, Yasny IE, Shuster AM, Seredenin SB, Petrov AV, Seifu S, McAleer J, Willing A, Cuevas J (February 2014). "Treatment with afobazole at delayed time points following ischemic stroke improves long-term functional and histological outcomes". Neurobiol Dis. 62: 354–364. doi:10.1016/j.nbd.2013.10.011. PMID 24141021.