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Fabomotizole

From Wikipedia, the free encyclopedia
Anxiolytic drug

Pharmaceutical compound
Fabomotizole
Clinical data
Trade namesAfobazole
Other namesObenoxazine
Routes of
administration
Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability43.64%, pronouncedfirst-pass effect
Metabolismextensive hepatic
Onset of action0.85±0.13 hours
Eliminationhalf-life0.82±0.54 hours
Identifiers
  • 4-[2-[(6-ethoxy-1H-benzimidazol-2-yl)sulfanyl]ethyl]morpholine
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC15H21N3O2S
Molar mass307.41 g·mol−1
3D model (JSmol)
  • CCOc3ccc2nc(SCCN1CCOCC1)[nH]c2c3
  • 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) checkY
  • Key:WWNUCVSRRUDYPP-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)
Afobazole from Russia

Fabomotizole (INN;[1] brand nameAfobazole) is ananxiolyticdrug launched in Russia in the early 2000s. It producesanxiolytic andneuroprotective effects without anysedative ormuscle relaxant actions.[citation needed] Itsmechanism of action remains poorly defined however, withGABAergic,NGF- andBDNF-release-promoting,MT1receptor agonism,MT3receptor antagonism, andsigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement withserotonin 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 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

[edit]

References

[edit]
  1. ^"International Nonproprietary Names for Pharmaceutical Substances (INN)"(PDF).WHO Drug Information.26 (1): 63. 2012. Retrieved21 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.
5-HT1ARTooltip 5-HT1A receptoragonists
GABAARTooltip GABAA receptorPAMsTooltip positive allosteric modulators
Gabapentinoids
(α2δVDCCblockers)
Antidepressants
Sympatholytics
(Antiadrenergics)
Others
MT1Tooltip Melatonin receptor 1
MT2Tooltip Melatonin receptor 2
Unsorted
σ1
σ2
Unsorted
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