Tìm theo
Olopatadine
Các tên gọi khác (5 ) :
  • Olopatadin
  • Olopatadina
  • Olopatadine
  • Olopatadinum
  • Opatanol
histamine h1 antagonists, histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 113806-05-6
ATC: S01GX09, R01AC08
ĐG : Alcon Laboratories , http://www.alcon.com
CTHH: C21H23NO3
PTK: 337.4122
Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
Phân tử khối
337.4122
Monoisotopic mass
337.167793607
InChI
InChI=1S/C21H23NO3/c1-22(2)11-5-8-18-17-7-4-3-6-16(17)14-25-20-10-9-15(12-19(18)20)13-21(23)24/h3-4,6-10,12H,5,11,13-14H2,1-2H3,(H,23,24)/b18-8-
InChI Key
InChIKey=JBIMVDZLSHOPLA-LSCVHKIXSA-N
IUPAC Name
2-[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-5-yl]acetic acid
Traditional IUPAC Name
[(2Z)-2-[3-(dimethylamino)propylidene]-9-oxatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-5-yl]acetic acid
SMILES
CN(C)CC\C=C1\C2=CC=CC=C2COC2=C1C=C(CC(O)=O)C=C2
Độ tan chảy
248 °C
Độ hòa tan
Soluble
logP
3.4
logS
-4
pKa (strongest acidic)
3.78
pKa (Strongest Basic)
9.76
PSA
49.77 Å2
Refractivity
109.55 m3·mol-1
Polarizability
37.44 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells.
Cơ Chế Tác Dụng : Used to treat allergic conjunctivitis (itching eyes), olopatadine inhibits the release of histamine from mast cells. It is a relatively selective histamine H1 antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells. Olopatadine is a selective histamine H1 antagonist that 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. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors.
Dược Động Học :
▧ Absorption :
Ophthalmic use of olopatadine usually does not produce measurable plasma concentrations.
▧ Metabolism :
The mono-desmethyl and the N-oxide metabolites have been detected at low concentrations in the urine.
▧ Route of Elimination :
Elimination was predominantly through renal excretion.
▧ Half Life :
3 hours
Chỉ Định : For the treatment of ocular itching associated with allergic conjunctivitis.
Liều Lượng & Cách Dùng : Liquid - Ophthalmic
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
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    Sản phẩm biệt dược : Alchek
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    Sản phẩm biệt dược : Alerchek
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    Sản phẩm biệt dược : Allelock
  • Công ty : Alcon
    Sản phẩm biệt dược : Opatanol
  • Công ty : Alcon
    Sản phẩm biệt dược : Pataday
  • Công ty : Alcon
    Sản phẩm biệt dược : Patanase
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  • Công ty : Alcon
    Sản phẩm biệt dược : Patanol S
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