Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H21N3O2S |
Molecular Weight | 307.411 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOC1=CC2=C(NC(SCCN3CCOCC3)=N2)C=C1
InChI
InChIKey=WWNUCVSRRUDYPP-UHFFFAOYSA-N
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)
Molecular Formula | C15H21N3O2S |
Molecular Weight | 307.411 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
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Target ID: CHEMBL287 |
5.9 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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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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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 |
PubMed
Title | Date | PubMed |
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[Pharmacological regulation of emotional stress reactions]. | 2003 |
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[Afobazole increases cerebral blood flow in rats with global brain ischemia]. | 2004 Sep-Oct |
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[Aphobazol--new selective anxyolytic drug]. | 2005 |
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[Using aphobazol for treatment of the emotional stress after exposure to ionizing radiation]. | 2005 Apr-Jun |
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Neuroprotective properties of afobazol in vitro. | 2005 Aug |
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[Evidence for the neuroprotective properties of afobazole in experimental model of focal brain ischemia]. | 2006 Jul-Aug |
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[A comparative study of the effect of afobazole on brain monoamine systems in BALB/C and C57BL/6 mice]. | 2006 Sep-Oct |
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[Pharmacokinetics of afobazole in rats]. | 2007 Mar-Apr |
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[Using of aphobazol in the treatment of adaptation disorder in the contract service men, dismissed from the armed forces]. | 2007 Nov |
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Excretion of afobazole and its metabolites with urine and feces in rats. | 2008 Apr |
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[Afobazole metabolism in rats]. | 2008 Mar-Apr |
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[Neuroprotective effects of afobazole in a hemorrhagic stroke model]. | 2009 Jan-Feb |
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[Selective anxiolytic afobazole increases the content of BDNF and NGF in cultured hippocampal HT-22 line neurons]. | 2009 Jan-Feb |
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[Afobazole effect on cerebral circulation under hemorrhagic stroke model conditions]. | 2009 Nov-Dec |
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Effect of afobazole on genotoxic effects of tobacco smoke in the placenta and embryonic tissues of rats. | 2010 Sep |
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[Anxiolytic afobazole action self-evaluated by patients with anxiety-asthenic disorders]. | 2010 Sep |
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.
Substance Class |
Chemical
Created
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admin
on
Edited
Sat Dec 16 17:50:01 GMT 2023
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Sat Dec 16 17:50:01 GMT 2023
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Record UNII |
0F8K1X115C
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Record Status |
Validated (UNII)
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N05BX04
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