Terfenadine 特非那定

CAS 50679-08-8 MFCD00079622

化学结构图

50679-08-8
SMILES: CC(C)(C)C1C=CC(=CC=1)C(O)CCCN1CCC(CC1)C(O)(C1C=CC=CC=1)C1C=CC=CC=1

化学属性

Mol. FormulaC32H41NO2
Mol. Weight471.67
TSCANo
Melting Point145-152°

别名和识别编码

Chemical NameTerfenadine
CAS Number50679-08-8
Synonym Terfen α-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol MDL 9918 Seldane Terfenadine Triludan Aldaban RMI 9918 Allerplus Terdin Nebralin alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol Teldane ?-[4-(1,1-Dmethylethyl)phenyl]-4-(hydroxydiphenylmethyl)- Teldanex
MDL NumberMFCD00079622
PubChem Substance ID24277779
EC Number256-710-8
Merck Number14,9163
Wiswesser Line NotationT6NTJ A3YQR DX1&1&1& DXQR&R
Beilstein Registry Number5857899
Chemical Name Translation特非那定
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分类

  • Pharmaceuticals
  • {SNA} Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Cell Signaling Enzymes, Drug and Xenobiotic Metabolism, Fluorination Ready Pharma-Developed Compounds, Multi-Drug Resistance and Drug Metabolism, Sanofi Aventis, Substrates, Inducers, Inhibitors, T, Xenobiotics And Drug Metabolism Substrates, Xenobiotics and Drug Metabolism, 生化试剂, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学, 酶、抑制剂和底物
  • {SNA} Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Cell Signaling Enzymes, Drug and Xenobiotic Metabolism, Fluorination Ready Pharma-Developed Compounds,

产品应用

  • Nonsedating-type histamine H1-receptor antagonist. Antihistaminic.

相关文献及参考

  • [2]. Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cells through ROS-dependent and -independent mechanisms. Apoptosis. 2011 Dec;16(12):1253-67.
  • [3]. An L, et al. Terfenadine combined with epirubicin impedes the chemo-resistant human non-small cell lung cancer both in vitro and in vivo through EMT and Notch reversal. Pharmacol Res. 2017 Oct;124:105-115.
  • Badwan, A.A., et al.: Anal. Profiles Drug Subs., 19, 627 (1990),
  • Carr, A.A., et al.: Arzneim. Forsch., 32, 1157 (1982),
  • Masheter, H.C., et al.: Clin. Rev. Allergy, 11, 5 (1993),
  • [1]. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307.
  • [1]. Kamiya K, et al. Molecular determinants of hERG channel block by terfenadine and cisapride. J Pharmacol Sci. 2008 Nov;108(3):301-307.
  • [2]. Nicolau-Galmés F, et al. Terfenadine induces apoptosis and autophagy in melanoma cell

安全信息

WGK Germany2
RTECSTM4969000 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 190 mg/kg/23W-I
TOXIC EFFECTS :
   Behavioral - muscle weakness
   Liver -

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - child
DOSE/DURATION           : 3 mg/kg
TOXIC EFFECTS :
   Skin and Appendages - dermatitis, other (after systemic exposure)
   Immunological Including Allergic - other immediate (humoral): urticaria,
   allergic rhinitis, serum sickness
REFERENCE :
   BMJOAE British Medical Journal.  (British Medical Assoc., BMA House,
   Tavistock Sq., London WC1H 9JR, UK)  V.1-    1857- Volume(issue)/page/year:
   293,536,1986

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 246 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   IYKEDH Iyakuhin Kenkyu.  Study of Medical Supplies.  (Nippon Koteisho
   Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan)  V.1- 1970- 
   Volume(issue)/page/year: 21,319,1990

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intraperitoneal
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 154 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   IYKEDH Iyakuhin Kenkyu.  Study of Medical Supplies.  (Nippon Koteisho
   Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan)  V.1- 1970- 
   Volume(issue)/page/year: 21,319,1

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human
DOSE/DURATIO

TYPE OF TEST            : TDL

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 17100 mg/kg
SEX/DURATION            : female 14 day(s) pre-mating  - 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - weaning or lactation index (e.g., #
   alive at weaning per # alive at day 4)
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 32,1179,1982

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 8550 mg/kg
SEX/DURATION            : female 14 day(s) pre-mating  - 21 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 32,1179,1982

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 8400 mg/kg
SEX/DURATION            : female 14 day(s) pre-mating
                          female 1-14 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Fertility - pre-implantation mortality (e.g. reduction in
   number of implants per female; total number of implants per corpora lutea)
   Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
   resorbed implants per total number of implants)
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 32,1179,1982

TYPE OF TEST

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. T - Bioactive Small Molecules
  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. Sanofi Aventis - Approved Therapeutics/Drug Candidates
  1. Chemical Synthesis 化学合成
  2. Building Blocks 合成砌块
  3. Heterocyclic Building Blocks 杂环合成砌块
  4. Homopiperidines 同哌啶
  1. Chemical Synthesis 化学合成
  2. Building Blocks 合成砌块
  3. Heterocyclic Building Blocks 杂环合成砌块
  4. Piperidines 哌啶
  1. Life Science 生命科学
  2. Biochemicals and Reagents 生化试剂
  3. Enzymes, Inhibitors, and Substrates - Biochemicals and Reagents
  4. Application Index - Enzymes, Inhibitors, and Substrates
  5. Cell Signaling Enzymes - Application Index
  6. Xenobiotics and Drug Metabolism - Cell Signaling Enzymes
  7. Substrates - Xenobiotics and Drug Metabolism
  1. Life Science 生命科学
  2. Cell Biology 细胞生物学
  3. Cell Signaling and Neuroscience - Cell Biology
  4. Multi-Drug Resistance and Drug Metabolism - Cell Signaling and Neuroscience
  5. Drug and Xenobiotic Metabolism - Multi-Drug Resistance and Drug Metabolism
  6. Substrates, Inducers, Inhibitors - Drug and Xenobiotic Metabolism
  1. Life Science 生命科学
  2. Biochemicals and Reagents
  3. Cell Signaling and Neuroscience
  4. Multi-Drug Resistance and Drug Metabolism
  5. Drug and Xenobiotic Metabolism
  1. Life Science 生命科学
  2. Biochemicals and Reagents
  3. Enzymes, Inhibitors, and Substrates
  4. Cell Signaling Enzymes
  5. Xenobiotics and Drug Metabolism
  6. Inhibitors
  1. Medical Research Areas
  2. GPCR & G Protein
  3. Histamine Receptor  (组胺受体)

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