Ebastine 依巴斯汀

CAS 90729-43-4 MFCD00865661

化学结构图

90729-43-4
SMILES: CC(C)(C)C1C=CC(=CC=1)C(=O)CCCN1CCC(CC1)OC(C1C=CC=CC=1)C1C=CC=CC=1

化学属性

Mol. FormulaC32H39NO2
Mol. Weight469.67
TSCANo
Melting Point85.0 to 89.0 deg-C

别名和识别编码

Chemical NameEbastine
CAS Number90729-43-4
Synonym 1-(4-(1,1-Dimethylethyl)phenyl)-4-(4-(diphenylmethoxy)-1-piperidinyl)-1-butanone 1-[4-(1,1-Dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone 4'-tert-Butyl-4-(4-(diphenylmethoxy)piperidino)butyrophenone 4-Diphenylmethoxy-1-(3-(4-tert-butylbenzoyl)propyl)piperidine Ebastel Ebastin Ebastina Ebastine Estivan Kestine LAS W-090 LAS-W 090 RP 64305
MDL NumberMFCD00865661
Merck Number3484
PubChem Substance ID160871155
Chemical Name Translation依巴斯汀
Reaxys-RN7522103
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分类

  • Pharmaceuticals
  • {SNA} Antagonists, Bioactive Small Molecules, Biochemicals and Reagents, 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
  • Intermediates & Fine Chemicals,
  • {SNA} Antagonists, Bioactive Small Molecule Alphabetical Index, E, GPCR Modulators, GPCR Proteins, Modulators and Antibodies, Histaminergics, Histaminergics - Antagonists, Membrane Protein Biology Tools, Neuroscience,

产品应用

  • A nonsedating type histamine H1-receptor antagonist. Antihistaminic.

相关文献及参考

  • [2]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503.
  • [3]. Fujii, et al. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38.
  • Carvajal, A., et al.: Clin. Pharmacol. Ther., 85, 481 (2009),
  • Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009),
  • Inomata, N., et al.: J. Dermatol., 36, 224 (2009),
  • [1]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20.
  • [1]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20.
  • [2]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503.
  • {MC

安全信息

RTECSEL8140000
Hazard statements
  • H413 Maycauselonglastingharmfuleffectstoaquaticlife 可能对水生生物造成长期持续有害影响。
WGK Germany3
Personal Protective Equipment Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Mammal - species unspecified
DOSE/DURATION           : 500 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   DRFUD4 Drugs of the Future.  (J.R. Prous, S.A., Apartado de Correos 540,
   08080 Barcelona, Spain) V.1-    1975/76-  Volume(issue)/page/year:
   15,674,1990

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - species unspecified
DOSE/DURATION           : >4 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   DRFUD4 Drugs of the Future.  (J.R. Prous, S.A., Apartado de Correos 540,
   08080 Barcelona, Spain) V.1-    1975/76-  Volume(issue)/page/year:
   15,674,1990

{hazard_c

{hazard_com

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >160 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   MDACAP Medicamentos de Actualidad.  (J.R. Prous, S.A., Apartado de Correos
   540, 08080 Barcelona, Spain)  V.1-    1965-  Volume(issue)/page/year:
   28(Suppl B),45,1992

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 22,1143,1994

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

{hazard_

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 3300 mg/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Embryo or Fetus - other effects to embryo
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 12600 mg/kg
SEX/DURATION            : male 9 week(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
   accessory glands
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 22,1179,1994

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 5 gm/kg
SEX/DURATION            : female 17-21 day(s) after conception
                          lactating female 20 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Maternal Effects - ovaries, fallopian tubes
   Reproductive - Maternal Effects - uterus, cervix, vagina
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
   YACHDS Yakuri to Chiryo.  Pharmacology and Therapeutics.  (Raifu Saiensu
   Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan)  V.1-    1972-
   Volume(issue)/page/year: 22,1217,1994

系列性分类

  1. Life Science 生命科学
  2. Cell Biology 细胞生物学
  3. Bioactive Small Molecules - Cell Biology
  4. E - Bioactive Small Molecules
  1. Medical Research Areas
  2. GPCR & G Protein
  3. Histamine Receptor  (组胺受体)

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