Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C15H21N3O2S.2ClH |
| Molecular Weight | 380.333 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CCOC1=CC2=C(C=C1)N=C(N2)SCCN3CCOCC3
InChI
InChIKey=OFMVMQZFMVQDFO-UHFFFAOYSA-N
InChI=1S/C15H21N3O2S.2ClH/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);2*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
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 |
|||
| 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 |
|||
| 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 |
|||
| 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 |
|||
| 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 |
|---|---|---|
| [State of hemopoiesis under exposure to low doses of ionizing radiation and emotional stress during treatment with anxiolytic aphobazole]. | 2001 Jan-Feb |
|
| [Effect of novel anxiolytic agent aphobazole on coherence of the brain biopotentials in MR and MNRA rats]. | 2001 Jul-Aug |
|
| [Clinical study of the selective anxiolytic agent afobazol]. | 2001 Mar-Apr |
|
| [Pharmacological regulation of emotional stress reactions]. | 2003 |
|
| Effect of noopept and afobazole on the development of neurosis of learned helplessness in rats. | 2003 Aug |
|
| [Pharmacological correction of emotional stress after exposure to ionizing radiation and treatment with a radioprotector indralin]. | 2003 Jan-Feb |
|
| [Comparative electroencephalographic evaluation of anxiolytics afobazol and diazepam in MR and MNRA inbred rats with different anxiety levels]. | 2003 Mar-Apr |
|
| [Afobazole increases cerebral blood flow in rats with global brain ischemia]. | 2004 Sep-Oct |
|
| [Aphobazol--new selective anxyolytic drug]. | 2005 |
|
| [Using aphobazol for treatment of the emotional stress after exposure to ionizing radiation]. | 2005 Apr-Jun |
|
| Neuroprotective properties of afobazol in vitro. | 2005 Aug |
|
| [Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon]. | 2005 Jan-Feb |
|
| Neuroprotective effects of afobazol in experimental cerebral hemorrhage. | 2005 Nov |
|
| [Effect of afobazole on transmembrane ion currents in mollusk neurons]. | 2005 Sep-Oct |
|
| Studies of long-term noopept and afobazol treatment in rats with learned helplessness neurosis. | 2006 Aug |
|
| [Effect of afobazole on the accumulation of free radical oxidation products and the catalase activity in rats with cerebral ischemia]. | 2006 Jul-Aug |
|
| [Evidence for the neuroprotective properties of afobazole in experimental model of focal brain ischemia]. | 2006 Jul-Aug |
|
| [Effect of afobazole on brain-ischemia-induced anxiety in rats]. | 2006 Mar-Apr |
|
| [A comparative study of the effect of afobazole on brain monoamine systems in BALB/C and C57BL/6 mice]. | 2006 Sep-Oct |
|
| [Psychopharmacotherapy of anxiety disorders in patients with cardio-vascular diseases: the use of aphobazole]. | 2007 |
|
| In vivo effects of afobazole (2-mercaptobenzimidazole derivative) on the 7,12-dimethylbenz [alpha]anthracene-induced oncogene and suppressor gene expression. | 2007 Nov-Dec |
|
| [Efficacy of aphobazole in the treatment of anxiety disorders in patients with chronic cerebro-vascular insufficiency]. | 2008 |
|
| Gateways to clinical trials. December 2008. | 2008 Dec |
|
| Neuroprotective effect of afobazole on rats with bilateral local photothrombosis of vessels in the prefrontal cortex. | 2008 Feb |
|
| [Antimutagenic and antiteratogenic properties of afobazole]. | 2009 Jan-Feb |
|
| [Effects of afobazole on the stress protein HSP70 level in the brain tissue of rats with global transient ischemia]. | 2009 Jan-Feb |
|
| [Neuroprotective effects of afobazole in a hemorrhagic stroke model]. | 2009 Jan-Feb |
|
| [Afobazole influence on antinociceptive properties of morphine]. | 2009 Jan-Feb |
|
| Interaction of afobazole with sigma1-receptors. | 2009 Jul |
|
| Effect of afobazole on mitochondrial monoamine oxidase A activity in vitro. | 2009 Jul |
|
| Effect of afobazole on DNA damage in patients with systemic lupus erythematosus. | 2009 Oct |
|
| [Effects of afobasol in the reperfusion arrhythmia model]. | 2010 |
|
| Neuroprotective properties of afobazole in repeated hemorrhagic stroke modeling in aged rats. | 2010 Aug |
|
| [Comparative study of the interoceptive effects of afobazole and diazepam]. | 2010 Oct |
|
| Comparative analysis of tissue availability for afobazole and compound M-11. | 2010 Sep |
|
| On the mechanism of antifibrillatory effect of afobazole. | 2010 Sep |
|
| Effect of afobazole on genotoxic effects of tobacco smoke in the placenta and embryonic tissues of rats. | 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
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
189638-30-0
Created by
admin on Sat Dec 16 10:05:04 GMT 2023 , Edited by admin on Sat Dec 16 10:05:04 GMT 2023
|
PRIMARY | |||
|
N5HRG2433S
Created by
admin on Sat Dec 16 10:05:04 GMT 2023 , Edited by admin on Sat Dec 16 10:05:04 GMT 2023
|
PRIMARY | |||
|
11349505
Created by
admin on Sat Dec 16 10:05:04 GMT 2023 , Edited by admin on Sat Dec 16 10:05:04 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
