Epinastine Hydrochloride 依匹斯汀盐酸盐

CAS 108929-04-0 MFCD00933434

化学结构图

108929-04-0
SMILES: Cl.NC1=NCC2C3C=CC=CC=3CC3C=CC=CC=3N12

化学属性

Mol. FormulaC16H16ClN3
Mol. Weight286
Melting Point275

别名和识别编码

Chemical NameEpinastine Hydrochloride
CAS Number108929-04-0
Synonym 9,13b-Dihydro-1H-dibenz[cf]imidazo[1,5-a]azepine hydrochloride WAL-801Cl 3-Amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine hydrochloride Elestat 3-Amino-9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepine hydrochloride Alesion Epinastine hydrochloride WAL 801 CL WAL 801CL
PubChem Substance ID87561223
MDL NumberMFCD00933434
Chemical Name Translation依匹斯汀盐酸盐
Reaxys-RN3576207
Beilstein Registry Number3576207
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分类

  • Bases & Related Reagents
  • Nucleotides
  • Heterocycles
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • {SNA} Antagonists, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents, Boehringer Ingelheim, Cell Biology, Cell Signaling and Neuroscience, E, GPCR Modulators, GPCR Proteins, Modulators and Antibodies, Histaminergics, Histaminergics - Antagonists, Membrane Protein Biology Tools, Neuroscience, Neurotransmission, Neurotransmitters, Proteins and Derivatives

产品应用

  • A tetracyclic, non-sedating histamine H1 receptor antagonist. Antihistaminic.

相关文献及参考

  • [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.
  • Ohshima, E., et al.: J. Med. Chem., 35, 2074 (1992),
  • Walther, G., et al.: Arzneim.-Forsch., 40, 440 (1990),
  • [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.
  • [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 i

安全信息

GHS Symbol
WGK Germany3
Hazard statements
  • H301 Toxic if swallowed 吞食有毒
Personal Protective Equipment Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
RTECSHO4360000
Precautionary statements
Signal word
Safety Statements
  • S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时，立即求医（可能时出示标签）；
Hazard Codes T
Risk Statements
  • R25 Toxic if swallowed 吞咽有毒
Storage condition 0-10 0-10°C 
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

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
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
SPECIES OBSERVED        : Rodent - rabbit
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

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
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

UN Number
Packing GroupIII

系列性分类

  1. Life Science 生命科学
  2. Cell Biology 细胞生物学
  3. Cell Signaling and Neuroscience - Cell Biology
  4. Approved Therapeutics/Drug Candidates - Cell Signaling and Neuroscience
  5. Boehringer Ingelheim - Approved Therapeutics/Drug Candidates
  1. Medical Research Areas
  2. GPCR & G Protein
  3. Histamine Receptor  (组胺受体)

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