Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H21N3O2S.ClH |
| Molecular Weight | 343.872 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCOC1=CC=C2N=C(NC2=C1)SCCN3CCOCC3
InChI
InChIKey=MYSRFAUFQZYTOV-UHFFFAOYSA-N
InChI=1S/C15H21N3O2S.ClH/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);1H
DescriptionCurator's Comment: description was created based on several sources, including http://pro-pharma.biz/?page_id=171
Curator's Comment: description was created based on several sources, including http://pro-pharma.biz/?page_id=171
Fabomotizole (also known as Afobazole) is a selective non-benzodiazepine anxiolytic which was developed in Russia and launched in 2006. The drug is used for the treatment of wide range of diseases: generalized anxious disorders, neurasthenia, adaptation disorders, sleep disorders, for alleviation of withdrawal syndrome. According to the drug label (in Russian), its action is related to the interaction with sigma-1 receptors.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL287 |
5.9 µM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | AFOBAZOLE Approved UseTo treat generalized anxious disorders, neurasthenia, adaptation disorders at patients with dermatological, oncologic, somatic (bronchial asthma, syndrome of innervated intestinal tract, system lupus erythematosus, ischemic heart disease, arterial hypertension, arrhythmia) diseases. In combination of complex therapy of sleep disorders related to anxiety, neurocirculatory asthenia, premenstrual syndrome, for alleviation of state at smoking withdrawal symptoms. Launch Date2006 |
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| Primary | AFOBAZOLE Approved UseTo treat generalized anxious disorders, neurasthenia, adaptation disorders at patients with dermatological, oncologic, somatic (bronchial asthma, syndrome of innervated intestinal tract, system lupus erythematosus, ischemic heart disease, arterial hypertension, arrhythmia) diseases. In combination of complex therapy of sleep disorders related to anxiety, neurocirculatory asthenia, premenstrual syndrome, for alleviation of state at smoking withdrawal symptoms. Launch Date2006 |
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| Primary | AFOBAZOLE Approved UseTo treat generalized anxious disorders, neurasthenia, adaptation disorders at patients with dermatological, oncologic, somatic (bronchial asthma, syndrome of innervated intestinal tract, system lupus erythematosus, ischemic heart disease, arterial hypertension, arrhythmia) diseases. In combination of complex therapy of sleep disorders related to anxiety, neurocirculatory asthenia, premenstrual syndrome, for alleviation of state at smoking withdrawal symptoms. Launch Date2006 |
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| Primary | AFOBAZOLE Approved UseTo treat generalized anxious disorders, neurasthenia, adaptation disorders at patients with dermatological, oncologic, somatic (bronchial asthma, syndrome of innervated intestinal tract, system lupus erythematosus, ischemic heart disease, arterial hypertension, arrhythmia) diseases. In combination of complex therapy of sleep disorders related to anxiety, neurocirculatory asthenia, premenstrual syndrome, for alleviation of state at smoking withdrawal symptoms. Launch Date2006 |
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| Palliative | AFOBAZOLE Approved UseTo treat generalized anxious disorders, neurasthenia, adaptation disorders at patients with dermatological, oncologic, somatic (bronchial asthma, syndrome of innervated intestinal tract, system lupus erythematosus, ischemic heart disease, arterial hypertension, arrhythmia) diseases. In combination of complex therapy of sleep disorders related to anxiety, neurocirculatory asthenia, premenstrual syndrome, for alleviation of state at smoking withdrawal symptoms. Launch Date2006 |
Doses
| Dose | Population | Adverse events |
|---|---|---|
60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Other AEs: Sleep disturbance, Anxiety... Other AEs: Sleep disturbance (9.7%) Sources: Anxiety (8.6%) Drowsiness (7.5%) Headache (5.4%) Irritability (3.2%) Hypertonia (2.7%) Hypotonia (1.6%) Dry mouth (1.6%) Muscle weakness (1.6%) Nausea (1.1%) Lumbar pain (0.5%) Tremor (0.5%) Disturbances of accommodation (0.5%) Frequent urination (0.5%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Disturbances of accommodation | 0.5% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Frequent urination | 0.5% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Lumbar pain | 0.5% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Tremor | 0.5% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Nausea | 1.1% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Dry mouth | 1.6% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Hypotonia | 1.6% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Muscle weakness | 1.6% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Hypertonia | 2.7% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Irritability | 3.2% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Headache | 5.4% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Drowsiness | 7.5% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Anxiety | 8.6% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
| Sleep disturbance | 9.7% | 60 mg 3 times / day multiple, oral Highest studied dose Dose: 60 mg, 3 times / day Route: oral Route: multiple Dose: 60 mg, 3 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 3.0 |
inconclusive [IC50 18.9991 uM] | |||
Page: 4.0 |
inconclusive [IC50 37.9083 uM] | |||
Page: 3.0 |
yes [IC50 10.684 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 9 | 10 |
no |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Comparative study of the interoceptive effects of afobazole and diazepam]. | 2010-10 |
|
| Comparative analysis of tissue availability for afobazole and compound M-11. | 2010-09 |
|
| On the mechanism of antifibrillatory effect of afobazole. | 2010-09 |
|
| Effect of afobazole on genotoxic effects of tobacco smoke in the placenta and embryonic tissues of rats. | 2010-09 |
|
| [Anxiolytic afobazole action self-evaluated by patients with anxiety-asthenic disorders]. | 2010-09 |
|
| Neuroprotective properties of afobazole in repeated hemorrhagic stroke modeling in aged rats. | 2010-08 |
|
| Effects of selective anxiolytic afobazole on active caspase-3. | 2010-08 |
|
| [Model study of afobazole distribution in pregnant and lactating female rats and infant rat pups]. | 2010-08 |
|
| [Antiarrhythmic properties of afobazole and other 2-mercaptobensimidazole derivatives]. | 2010-05 |
|
| [Cerebrovascular effects of afobazole under conditions of combined disorders of cerebral and coronary circulation]. | 2010-05 |
|
| [Neurochemical study of effects of the new anxiolytic drugs afobazol and ladasten on the synthesis and metabolism of monoamines and their metabolites in the brain structures of Wistar rat on the model of monoamine synthesis blockade induced by aromatic amino acid decarboxylase inhibitor NSD-1015]. | 2010-03 |
|
| [Afobazole effect on cerebral circulation under hemorrhagic stroke model conditions]. | 2010-01-26 |
|
| [Effectiveness of combined application of ursosan and anxiolytic 2-mercaptobenzimidazole in early stage of cholelithiasis]. | 2010 |
|
| [Afobasol efficacy in a model of vagotonic atrial fibrillation]. | 2010 |
|
| [Afobasol antifibrillation activity in animals with the intact and denervated myocardium]. | 2010 |
|
| [Effects of afobasol in the reperfusion arrhythmia model]. | 2010 |
|
| Effect of afobazole on DNA damage in patients with systemic lupus erythematosus. | 2009-10 |
|
| Interaction of afobazole with sigma1-receptors. | 2009-07 |
|
| Effect of afobazole on mitochondrial monoamine oxidase A activity in vitro. | 2009-07 |
|
| [Antimutagenic and antiteratogenic properties of afobazole]. | 2009-04-02 |
|
| [Specific effects of selective anxiolytic afobazole on the cardiovascular system]. | 2009-04-02 |
|
| [Afobazole effect on heart rate variability in rats with different behaviors in the "open field" test]. | 2009-04-02 |
|
| [Effects of afobazole on the stress protein HSP70 level in the brain tissue of rats with global transient ischemia]. | 2009-04-02 |
|
| [Neuroprotective effects of afobazole in a hemorrhagic stroke model]. | 2009-04-02 |
|
| [Afobazole influence on antinociceptive properties of morphine]. | 2009-04-02 |
|
| [Antidepressant properties of afobazole in Porsolt and Nomura tests]. | 2009-04-02 |
|
| [Afobazole decreases motor side effects induced by haloperidol]. | 2009-04-02 |
|
| [Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons]. | 2009-04-02 |
|
| [Neuroreceptor mechanisms of the afobazole effect]. | 2009-04-02 |
|
| Gateways to clinical trials. December 2008. | 2008-12 |
|
| [Afobazole metabolism in rats]. | 2008-05-21 |
|
| Excretion of afobazole and its metabolites with urine and feces in rats. | 2008-04 |
|
| Effect of afobazole on teratogenic activity of cyclophosphamide in rats. | 2008-04 |
|
| Neuroprotective effect of afobazole on rats with bilateral local photothrombosis of vessels in the prefrontal cortex. | 2008-02 |
|
| In vivo effects of afobazole (2-mercaptobenzimidazole derivative) on the 7,12-dimethylbenz [alpha]anthracene-induced oncogene and suppressor gene expression. | 2008-01-24 |
|
| [Administration of afobasol for correction of mental disorders in celiac disease patients]. | 2008 |
|
| [Efficacy of aphobazole in the treatment of anxiety disorders in patients with chronic cerebro-vascular insufficiency]. | 2008 |
|
| [Using of aphobazol in the treatment of adaptation disorder in the contract service men, dismissed from the armed forces]. | 2007-11 |
|
| [Pharmacokinetics of afobazole in rats]. | 2007-05-26 |
|
| Tissue availability of afobazole and its major metabolites in rats. | 2007-05 |
|
| [Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole]. | 2007 |
|
| [A comparative study of the effect of afobazole on brain monoamine systems in BALB/C and C57BL/6 mice]. | 2006-12-13 |
|
| [Effect of afobazole on the accumulation of free radical oxidation products and the catalase activity in rats with cerebral ischemia]. | 2006-09-26 |
|
| [Evidence for the neuroprotective properties of afobazole in experimental model of focal brain ischemia]. | 2006-09-26 |
|
| [Effects of afobazole on the BDNF content in brain structures of inbred mice with different phenotypes of emotional stress reaction]. | 2006-08-02 |
|
| Studies of long-term noopept and afobazol treatment in rats with learned helplessness neurosis. | 2006-08 |
|
| [Effect of afobazole on brain-ischemia-induced anxiety in rats]. | 2006-07-19 |
|
| [Effect of afobazole on transmembrane ion currents in mollusk neurons]. | 2005-11-10 |
|
| Neuroprotective effects of afobazol in experimental cerebral hemorrhage. | 2005-11 |
|
| Neuroprotective properties of afobazol in vitro. | 2005-08 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: http://rupharma.com/afobazol/
For adult persons and children it is recommended to use internally, after meal. Usually it is recommended to use 1 tablet (10 mg) trice per day. The maximum daily dose is 60 mg. The period of therapy is 2-4 weeks. According to doctor prescription it is possible to prolong the period up to 3 months.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19334503
Experiments on immortalized hippocampal cell culture of mice showed that afobazole increases the NGF level in a final concentration of 10(-8) M and the BDNF level in final concentrations from 10(-8) to 10(-5) M.
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NCI_THESAURUS |
C28197
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Fabomotizole
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SUB37908
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ACTIVE MOIETY
SUBSTANCE RECORD