FABOMOTIZOLE

Possibly Marketed Outside US

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)

HIDE SMILES / InChI

Molecular Formula	C15H21N3O2S
Molecular Weight	307.411
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

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
Sigma opioid receptor 64	Agonist 2,752		5.9 µM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Generalized anxiety disorder 32	Primary	Approved 8,583	AFOBAZOLE
Neurasthenia 6	Primary	Approved 8,583	AFOBAZOLE
Adjustment disorder 3	Primary	Approved 8,583	AFOBAZOLE
Insomnia 111	Primary	Approved 8,583	AFOBAZOLE
Withdrawal syndrome 3	Palliative	Approved 8,583	AFOBAZOLE

Doses

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Dose	Population	Adverse events
60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT	Other AEs: Sleep disturbance, Anxiety...

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AEs

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AE	Significance	Dose	Population
Disturbances of accommodation	0.5%	60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Frequent urination	0.5%	60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Lumbar pain	0.5%	60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Tremor	0.5%	60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT
Nausea	1.1%	60 mg 3 times / day multiple, oral Highest studied dose	unhealthy, ADULT

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2,252	inhibitor 2,438	inhibitor 2,507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	P-gp 2,052

Drug as perpetrator

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Target	Modality	Activity
CYP2D6 2,546	inhibitor 4,027	inconclusive [IC50 18.9991 uM]
CYP2C9 2,497	inhibitor 4,027	inconclusive [IC50 37.9083 uM]
CYP3A4 2,633	inhibitor 4,027	yes [IC50 10.684 uM]

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Drug as victim

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Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2,052	substrate 4,014	no

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PubMed

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Title	Date	PubMed
Effect of noopept and afobazole on the development of neurosis of learned helplessness in rats.	2003 Aug	14631499
[Gabaergic mechanism of cerebrovascular and neuroprotective effects of afobazole and picamilon].	2005 Jan-Feb	15786959
[Effect of afobazole on transmembrane ion currents in mollusk neurons].	2005 Sep-Oct	16277200
[Evidence for the neuroprotective properties of afobazole in experimental model of focal brain ischemia].	2006 Jul-Aug	16995428
[A comparative study of the effect of afobazole on brain monoamine systems in BALB/C and C57BL/6 mice].	2006 Sep-Oct	17153957

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Patents

Sample Use Guides

In Vivo Use Guide

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

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
Record UNII	0F8K1X115C
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

FABOMOTIZOLE

Official Name

English

CM-346

Preferred Name

English

AFOBAZOLE

Common Name

English

1H-BENZIMIDAZOLE, 5-ETHOXY-2-((2-(4-MORPHOLINYL)ETHYL)THIO)-

Systematic Name

English

APHOBAZOLE

Common Name

English

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Classification Tree

Code System

Code

Other anxiolytics

WHO-ATC

N05BX04

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Code System

Code

Type

Description

EVMPD

SUB183842

PRIMARY

DRUG BANK

DB13623

PRIMARY

DRUG CENTRAL

4079

PRIMARY

EVMPD

SUB37908

PRIMARY

ChEMBL

CHEMBL3707307

PRIMARY

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					N5HRG2433S

FABOMOTIZOLE DIHYDROCHLORIDE

SALT/SOLVATE -> PARENT

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					HDO6HX6NZU

FABOMOTIZOLE HYDROCHLORIDE

SALT/SOLVATE -> PARENT

Amount:

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Related Record

Type

Details


					0F8K1X115C

FABOMOTIZOLE

ACTIVE MOIETY

Amount:

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SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

PubMed

Patents

Sample Use Guides

Drug as perpetrator