Tìm theo
Galantamine
Các tên gọi khác (2) :
  • (-)-Galanthamine
  • Galanthamine
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 357-70-0
ATC: N06DA04
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C17H21NO3
PTK: 287.3535
A benzazepine derived from norbelladine. It is found in galanthus and other amaryllidaceae. Galantamine is a cholinesterase inhibitor that has been used to reverse the muscular effects of gallamine triethiodide and tubocurarine, and has been studied as a treatment for Alzheimer's disease and other central nervous system disorders. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H21NO3
Phân tử khối
287.3535
Monoisotopic mass
287.152143543
InChI
InChI=1S/C17H21NO3/c1-18-8-7-17-6-5-12(19)9-14(17)21-16-13(20-2)4-3-11(10-18)15(16)17/h3-6,12,14,19H,7-10H2,1-2H3/t12-,14-,17-/m0/s1
InChI Key
InChIKey=ASUTZQLVASHGKV-JDFRZJQESA-N
IUPAC Name
(1S,12S,14R)-9-methoxy-4-methyl-11-oxa-4-azatetracyclo[8.6.1.0^{1,12}.0^{6,17}]heptadeca-6,8,10(17),15-tetraen-14-ol
Traditional IUPAC Name
galantamine
SMILES
[H][C@]12C[C@@H](O)C=C[C@]11CCN(C)CC3=C1C(O2)=C(OC)C=C3
Độ tan chảy
269-270 °C (HBr salt)
Độ hòa tan
10 mg/mL (HBr salt)
logP
1.8
logS
-2.2
pKa (strongest acidic)
14.81
pKa (Strongest Basic)
8.91
PSA
41.93 Å2
Refractivity
82.3 m3·mol-1
Polarizability
31.4 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Galantamine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. It is indicated for the treatment of mild to moderate dementia of the Alzheimer's type. An early pathophysiological feature of Alzheimer's disease that is associated with memory loss and cognitive deficits is a deficiency of acetylcholine as a result of selective loss of cholinergic neurons in the cerebral cortex, nucleus basalis, and hippocampus. Galantamine is postulated to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by acetylcholinesterase. If this proposed mechanism of action is correct, Galantamine's effect may lessen as the disease progresses and fewer cholinergic neurons remain functionally intact. There is no evidence that Galantamine alters the course of the underlying dementing process.
Cơ Chế Tác Dụng : A benzazepine derived from norbelladine. It is found in galanthus and other amaryllidaceae. Galantamine is a cholinesterase inhibitor that has been used to reverse the muscular effects of gallamine triethiodide and tubocurarine, and has been studied as a treatment for Alzheimer's disease and other central nervous system disorders. [PubChem] Galantamine is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor. It is not structurally related to other acetylcholinesterase inhibitors. Galantamine's proposed mechanism of action involves the reversible inhibition of acetylcholinesterase, which prevents the hydrolysis of acetycholine, leading to an increased concentration of acetylcholine at cholinergic synapses. Galantamine also binds allosterically with nicotinic acetylcholine receptors and may possibly potentiate the action of agonists (such as acetylcholine) at these receptors.
Dược Động Học :

▧ Volume of Distribution :
* 175 L
▧ Protein binding :
18%
▧ Route of Elimination :
Galantamine is metabolized by hepatic cytochrome P450 enzymes, glucuronidated, and excreted unchanged in the urine.
▧ Half Life :
7 hours
▧ Clearance :
* 300 mL/min [After IV. or oral administration]
Độc Tính : LD50=75 mg/kg (rat)
Chỉ Định : For the treatment of mild to moderate dementia of the Alzheimer's type. Has also been investigated in patients with mild cognitive impairment who did not meet the diagnostic criteria for Alzheimer's disease.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Capsule, extended release - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Lycoremine
  • Công ty :
    Sản phẩm biệt dược : Nivalin
  • Công ty :
    Sản phẩm biệt dược : Razadyne
  • Công ty :
    Sản phẩm biệt dược : Reminyl
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00674
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=908828
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505659
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08526
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04292
ChemSpider
http://www.chemspider.com/Chemical-Structure.23175565.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=10404
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-8104-91
PharmGKB
http://www.pharmgkb.org/drug/PA449726
Wikipedia
http://en.wikipedia.org/wiki/Galantamine
RxList
http://www.rxlist.com/cgi/generic/reminyl.htm
Drugs.com
http://www.drugs.com/cdi/galantamine.html
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