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分类

• {SNA} AN-AZ, Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Ion Channels, Johnson & Johnson, Monovalent Ion Channels, Other Sodium Channel Modulators, Sodium Channel Modulators, Voltage-gated Ion Channels, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
• Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Ion Channels, Johnson & Johnson, Monovalent Ion Channels, Other Sodium Channel Modulators, Sodium Channel Modulators, Voltage-gated Ion Channels
• {SNA} Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Ion Channels,

产品应用

• Nonsedating-type histamine H1-receptor antagonist. Potential for combination therapy with antivancer drugs such as doxorubicin in resistant leukemia. Antihistaminic.

相关文献及参考

• [2]. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61.
• ########
• Ficker, E., et al., The binding site for channel blockers that rescue misprocessed human long QT syndrome type 2 ether-a-gogo-related gene (HERG) mutations. J. Biol. Chem. 277 , 4989-4998, (2002)
• Merck 14 ,856
• Roy, J., et al., Pharmacological separation of hEAG and hERG K+ channel function in the human mammary carcinoma cell line MCF-7. Oncol. Rep. 19 , 1511-1526, (2008) 摘要
• Wang, L., et al., Intracellular potassium stabilizes hERG channels for export from endoplasmic reticulum. Mol. Pharmacol. , (2009)
• [1]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, as
• [1]. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21(2):294-300.

安全信息

GHS Symbol

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 4 mg/kg
TOXIC EFFECTS :
   Cardiac - change in rate
REFERENCE :
   JTCTDW Journal of Toxicology, Clinical Toxicology.  (Marcel Dekker, 270
   Madison Ave., New York, NY 10016)  V.19-    1982-  Volume(issue)/page/year:
   31,121,1993

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcu

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 5400 ug/kg
TOXIC EFFECTS :
   Behavioral - general anesthetic
   Cardiac - EKG changes not diagnostic of specified effects
   Cardiac - pulse rate increase, without fall in BP
REFERENCE :
   PECAE5 Pediatric Emergency Care.  (Williams & Wilkins, 428 E. Preston St.,
   Baltimore, MD  21202) V.1-    1985-  Volume(issue)/page/year: 9,23,1993

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 21800 ug/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 33,381,1983

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : 933 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans
   Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium)  V.4-   
   1898-  Volume(issue

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 220 mg/kg
SEX/DURATION            : female 1-22 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
   Reproductive - Effects on Newborn - behavioral
   Reproductive - Effects on Newborn - physical
REFERENCE :
   CBPCEE Comparative Biochemistry and Physiology, C: Pharmacology, Toxicology
   and Endocrinology. (Elsevier Science, 660 White Plains Rd., Tarrytown, NY
   10591)  V.74-    1983-  Volume(issue)/page/year: 114,123,1996