Epinastin HCl

Modify Date: 2024-01-02 10:14:54

Epinastin HCl Structure
Epinastin HCl structure
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 Chinese USA Flash Point 212.7ºC
Symbol GHS06
GHS06
Signal Word Danger

 Use of Epinastin HCl


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].

 Names

Name Epinastine Hydrochloride
Synonym More Synonyms

 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

 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
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

~90%

Epinastin HCl Structure

Epinastin HCl

CAS#:108929-04-0

Literature: USV LIMITED Patent: WO2009/63504 A2, 2009 ; Location in patent: Page/Page column 25 ;

~%

Epinastin HCl Structure

Epinastin HCl

CAS#:108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

~%

Epinastin HCl Structure

Epinastin HCl

CAS#:108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

~%

Epinastin HCl Structure

Epinastin HCl

CAS#:108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

~%

Epinastin HCl Structure

Epinastin HCl

CAS#:108929-04-0

Literature: Arzneimittel-Forschung/Drug Research, , vol. 40, # 4 p. 440 - 446

 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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 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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