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Pemirolast
Các tên gọi khác (5 ) :
  • Pemirolast
  • Pemirolast
  • Pemirolast
  • Pemirolastum
  • Pemirox
histamine antagonists, ophthalmics
Thuốc Gốc
Small Molecule
CAS: 100299-08-9
ĐG : Santen Inc. , http://www.santeninc.com
CTHH: C10H8N6O
PTK: 228.2101
Pemirolast potassium is a slightly yellow powder that is soluble in water. It is a mast cell stabilizer that acts as an antiallergic agent. As an ophthalmic aqueous sterile solution, pemirolast is used for the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis. Pemirolast is potentially useful for prophylaxis of pulmonary hypersensitivity reactions to drugs such as paclitaxel.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H8N6O
Phân tử khối
228.2101
Monoisotopic mass
228.075958908
InChI
InChI=1S/C10H8N6O/c1-6-3-2-4-16-9(6)11-5-7(10(16)17)8-12-14-15-13-8/h2-5H,1H3,(H,12,13,14,15)
InChI Key
InChIKey=HIANJWSAHKJQTH-UHFFFAOYSA-N
IUPAC Name
9-methyl-3-(2H-1,2,3,4-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one
Traditional IUPAC Name
pemirolast
SMILES
CC1=CC=CN2C(=O)C(=CN=C12)C1=NNN=N1
Độ hòa tan
4.62e-01 g/l
logS
-2.7
pKa (strongest acidic)
5.8
pKa (Strongest Basic)
-1.4
PSA
87.13 Å2
Refractivity
63.35 m3·mol-1
Polarizability
21.96 Å3
logP
0
Rotatable Bond Count
1
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Pemirolast is used for the prophylactic treatment of itching of the eye associated with allergic conjunctivitis. Pemirolast potassium is a mast cell stabilizer that inhibits the in vivo Type I immediate hypersensitivity reaction. Pemirolast inhibits the antigen-induced release of inflammatory mediators (e.g., histamine, leukotriene C4, D4, E4) from human mast cells. Allergic reactions lead to cell-degranulation and the release of histamine (and other chemical mediators) from the mast cell or basophil. Once released, histamine can react with local or widespread tissues through histamine receptors. Histamine, acting on H1-receptors, produces pruritis and vasodilatation (allowing blood fluids to enter the area to cause swelling). Pemirolast is a histamine H1 antagonist. It competes with histamine for the normal H1-receptor sites on effector cells of blood vessels to provide effective, temporary relief of watery and itchy eyes.
Cơ Chế Tác Dụng : Pemirolast potassium is a slightly yellow powder that is soluble in water. It is a mast cell stabilizer that acts as an antiallergic agent. As an ophthalmic aqueous sterile solution, pemirolast is used for the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis. Pemirolast is potentially useful for prophylaxis of pulmonary hypersensitivity reactions to drugs such as paclitaxel. Pemirolast binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine. Pemirolast has also been observed to inhibit antigen-stimulated calcium ion influx into mast cells through the blockage of calcium channels. Pemirolast inhibits the chemotaxis of eosinophils into ocular tissue, and prevents inflammatory mediator release from human eosinophils.
Dược Động Học :

▧ Metabolism :
Hepatic (Ophthalmic)
▧ Route of Elimination :
Following topical administration, about 10-15% of the dose was excreted unchanged in the urine.
▧ Half Life :
4.5 hours (Ophthalmic)
Chỉ Định : For the prevention of itching of the eyes caused by allergies such as hay fever, and allergic conjunctivitis
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Alamast 0.1% drops
    Giá bán buôn : USD >11.39
    Đơn vị tính : ml
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00885
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=57697
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509034
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01088
ChemSpider
http://www.chemspider.com/Chemical-Structure.51990.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/68669-711-10
PharmGKB
http://www.pharmgkb.org/drug/PA164781018
Wikipedia
http://en.wikipedia.org/wiki/Pemirolast
RxList
http://www.rxlist.com/cgi/generic/alamast.htm
Drugs.com
http://www.drugs.com/cdi/pemirolast.html
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