Epinastin HCl

Names

[ Name ]:
Epinastin HCl

[Synonym ]:
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

Biological Activity

[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 Receptor

Research Areas >> Endocrinology

Research Areas >> Inflammation/Immunology

Signaling 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

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
H2O: soluble38mg/mL

MSDS

Click to get detail MSDS

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

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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%

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Related Compounds

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