CAS 108929-04-0|Epinastin HCl

Introduction：Basic information about CAS 108929-04-0|Epinastin HCl, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Epinastin HCl BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles29
8. Synonyms

Common Name	Epinastin HCl
CAS Number	108929-04-0	Molecular Weight	285.771
Density	1.32g/cm3	Boiling Point	428ºC at 760 mmHg
Molecular Formula	C₁₆H₁₆ClN₃	Melting Point	>270ºC
MSDS	ChineseUSA	Flash Point	212.7ºC
Symbol	GHS06	Signal Word	Danger

Names

Name	Epinastine Hydrochloride
Synonym	More Synonyms

Epinastin HCl BiologicalActivity

Description	Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action[1][2][3].
Related Catalog	Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>EndocrinologyResearch Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor
References	[1]. C Kamei, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205. [2]. T Roeder, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. ur J Pharmacol. 1998 May 22;349(2-3):171-7. [3]. T Kohyama, et al. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8.

Description

Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action[1][2][3].

Related Catalog

Signaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>EndocrinologyResearch Areas >>Inflammation/ImmunologySignaling Pathways >>GPCR/G Protein >>Histamine Receptor

References

[1]. C Kamei, et al. Antiallergic effect of epinastine (WAL 801 CL) on immediate hypersensitivity reactions: (I). Elucidation of the mechanism for histamine release inhibition. Immunopharmacol Immunotoxicol. 1992;14(1-2):191-205.

[2]. T Roeder, et al. Epinastine, a highly specific antagonist of insect neuronal octopamine receptors. ur J Pharmacol. 1998 May 22;349(2-3):171-7.

[3]. T Kohyama, et al. A novel antiallergic drug epinastine inhibits IL-8 release from human eosinophils. Biochem Biophys Res Commun. 1997 Jan 3;230(1):125-8.

Chemical & Physical Properties

Density	1.32g/cm3
Boiling Point	428ºC at 760 mmHg
Melting Point	>270ºC
Molecular Formula	C₁₆H₁₆ClN₃
Molecular Weight	285.771
Flash Point	212.7ºC
Exact Mass	285.103271
PSA	41.62000
LogP	3.46970
Vapour Pressure	1.56E-07mmHg at 25°C
InChIKey	VKXSGUIOOQPGAF-UHFFFAOYSA-N
SMILES	Cl.NC1=NCC2c3ccccc3Cc3ccccc3N12
Storage condition	2-8°C
Water Solubility	H2O: soluble38mg/mL

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HO4360000

CHEMICAL NAME :: IH-Dibenz(c,f)imidazo(1,5-a)azepin-3-amine, 9,13b-dihydro-, hydrochloride

CAS REGISTRY NUMBER :: 108929-04-0

LAST UPDATED :: 199210

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C16-H15-N3.Cl-H

MOLECULAR WEIGHT :: 285.80

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 :: 192 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Gastrointestinal - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 13650 mg/kg/13W-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in endocrine weight (unspecified) Blood - changes in platelet count

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 36400 mg/kg/52W-C

TOXIC EFFECTS :: Behavioral - food intake (animal) Endocrine - changes in endocrine weight (unspecified) Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 42,151,1991 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 13 gm/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8400 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 975 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 41,355,1991

Safety Information

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301
Precautionary Statements	P301 + P310
Personal Protective Equipment	Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes	T: Toxic;
Risk Phrases	R25
Safety Phrases	45
RIDADR	UN 2811 6
RTECS	HO4360000
HS Code	2933990090

Customs

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles29

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J. Comp. Physiol. A. Neuroethol. Sens. Neural. Behav. Physiol. 195(3) , 265-77, (2009)

The biogenic amine, octopamine, modulates a variety of aspects of insect motor behavior, including direct action on the flight central pattern generator. A number of recent studies demonstrate that ty...

Synonyms

9,13b-Dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-aminhydrochlorid

UNII:GFM415S5XL

9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azépin-3-amine chlorhydrate

9,13b-Dihydro-1H-dibenz[cf]imidazo[1,5-a]azepine hydrochloride,WAL-801Cl

1H-Dibenz[c,f]imidazo[1,5-a]azepin-3-amine, 9,13b-dihydro-, hydrochloride (1:1)

3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine Hydrochloride

EPINASTINHCL

Epinastine hydrochloride

Epinastinehydrochloride

1H-Dibenz[c,f]imidazo[1,5-a]azepin-3-amine,9,13b-dihydro-,hydrochloride

T B5 G6&6 BN DN CUT&T&J CZ &&HCl

EPIMEDIUM P.E

EPINASTINE HCL

Epinastine

9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine hydrochloride

1H-DIBENZ[C,F]IMIDAZO[1,5-A]AZEPIN-3-AMINE,9,13B-DIHYDRO-, HYDROCHLORIDE (1:1)

9,13b-Dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine hydrochloride (1:1)

Epinastin HCl

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