CAS 21715-46-8|Etifoxine

Introduction：Basic information about CAS 21715-46-8|Etifoxine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Etifoxine BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Synonyms

Common Name	Etifoxine
CAS Number	21715-46-8	Molecular Weight	300.783
Density	1.2±0.1 g/cm3	Boiling Point	421.2±55.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₇ClN₂O	Melting Point	/
MSDS	/	Flash Point	208.5±31.5 °C

Names

Name	6-chloro-N-ethyl-4-methyl-4-phenyl-3,1-benzoxazin-2-amine
Synonym	More Synonyms

Etifoxine BiologicalActivity

Description	Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease
References	[1]. Verleye M, Dumas S, Heulard I, et al. Differential effects of etifoxine on anxiety-like behaviour and convulsions in BALB/cByJ and C57BL/6J mice: any relation to overexpression of central GABAA receptor beta2 subunits? Eur Neuropsychopharmacol. 2011 Jun;2 [2]. Bourin M, Hascot M. Implication of 5-HT2 receptor subtypes in the mechanism of action of the GABAergic compound etifoxine in the four-plate test in Swiss mice. Behav Brain Res. 2010 Apr 2;208(2):352-8. [3]. Gee KW, Tran MB, Hogenkamp DJ, et al. Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther. 2010 Mar;332(3):1040-53. [4]. Aouad M, Charlet A, Rodeau JL, et al. Reduction and prevention of vincristine-induced neuropathic pain symptoms by the non-benzodiazepine anxiolytic etifoxine are mediated by 3alpha-reduced neurosteroids. Pain. 2009 Dec 15;147(1-3):54-9. [5]. Girard C, Liu S, Cadepond F, et al. Etifoxine improves peripheral nerve regeneration and functional recovery. Proc Natl Acad Sci U S A. 2008 Dec 23;105(51):20505-10.

Description

Etifoxine(HOE 36-801) is potentiator of GABAA receptor function in cultured neurons. Etifoxine preferentially acts on β2 or β3 subunit-containing GABAA receptors. IC50 value:Target: GABAA receptorEtifoxine exhibits anxiolytic activity in rodents and humans with no sedative, myorelaxant or mnesic side effects. Etifoxine acts as a ligand of the translocator protein (TSPO); promotes axonal regeneration.

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>GABA ReceptorSignaling Pathways >>Neuronal Signaling >>GABA ReceptorResearch Areas >>Neurological Disease

References

[1]. Verleye M, Dumas S, Heulard I, et al. Differential effects of etifoxine on anxiety-like behaviour and convulsions in BALB/cByJ and C57BL/6J mice: any relation to overexpression of central GABAA receptor beta2 subunits? Eur Neuropsychopharmacol. 2011 Jun;2

[2]. Bourin M, Hascot M. Implication of 5-HT2 receptor subtypes in the mechanism of action of the GABAergic compound etifoxine in the four-plate test in Swiss mice. Behav Brain Res. 2010 Apr 2;208(2):352-8.

[3]. Gee KW, Tran MB, Hogenkamp DJ, et al. Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther. 2010 Mar;332(3):1040-53.

[4]. Aouad M, Charlet A, Rodeau JL, et al. Reduction and prevention of vincristine-induced neuropathic pain symptoms by the non-benzodiazepine anxiolytic etifoxine are mediated by 3alpha-reduced neurosteroids. Pain. 2009 Dec 15;147(1-3):54-9.

[5]. Girard C, Liu S, Cadepond F, et al. Etifoxine improves peripheral nerve regeneration and functional recovery. Proc Natl Acad Sci U S A. 2008 Dec 23;105(51):20505-10.

Chemical & Physical Properties

Density	1.2±0.1 g/cm3
Boiling Point	421.2±55.0 °C at 760 mmHg
Molecular Formula	C₁₇H₁₇ClN₂O
Molecular Weight	300.783
Flash Point	208.5±31.5 °C
Exact Mass	300.102936
PSA	33.62000
LogP	3.78
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.601
InChIKey	IBYCYJFUEJQSMK-UHFFFAOYSA-N
SMILES	CCN=C1Nc2ccc(Cl)cc2C(C)(c2ccccc2)O1

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DM3028000

CHEMICAL NAME :: 4H-3,1-Benzoxazine, 6-chloro-2-ethylamino-4-methyl-4-phenyl-

CAS REGISTRY NUMBER :: 21715-46-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C17-H17-Cl-N2-O

MOLECULAR WEIGHT :: 300.81

WISWESSER LINE NOTATION :: T66 BN DO EHJ CM2 E1 ER& HG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 292 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 55 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1388 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 133 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 27,325,1972

Safety Information

HS Code	2934999090

Customs

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

Etifoxine

Etifoxina [Spanish]

4H-3,1-Benzoxazin-2-amine, 6-chloro-N-ethyl-4-methyl-4-phenyl-

6-Chloro-N-ethyl-4-methyl-4-phenyl-4H-3,1-benzoxazin-2-amine

Etifoxina [INN-Spanish]

Etifoxinum [INN-Latin]

Etifoxinum [Latin]

(6-chloro-4-methyl-4-phenyl-4H-benzo[d][1,3]oxazin-2-yl)-ethyl-amine

Etifoxin

rac-etifoxine

Etafenoxine

stresam

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