Tìm theo
Varenicline
Các tên gọi khác (1) :
  • CP-526,555
nicotinic agonists
Thuốc Gốc
Small Molecule
CAS: 249296-44-4
ATC: N07BA03
ĐG : Cardinal Health , http://www.cardinal.com
CTHH: C13H13N3
PTK: 211.2624
Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H13N3
Phân tử khối
211.2624
Monoisotopic mass
211.110947431
InChI
InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2/t8-,9+
InChI Key
InChIKey=JQSHBVHOMNKWFT-DTORHVGOSA-N
IUPAC Name
(1R,12S)-5,8,14-triazatetracyclo[10.3.1.0^{2,11}.0^{4,9}]hexadeca-2(11),3,5,7,9-pentaene
Traditional IUPAC Name
varenicline
SMILES
[H][C@]12C[C@]([H])(CNC1)C1=CC3=NC=CN=C3C=C21
Độ hòa tan
8.77e-02 g/l
logP
0.9
logS
-3.4
pKa (Strongest Basic)
9.73
PSA
37.81 Å2
Refractivity
61.3 m3·mol-1
Polarizability
23.12 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Varenicline is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain.
Cơ Chế Tác Dụng : Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors. Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectiviyty for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.
Dược Động Học :

▧ Protein binding :
Less than 20%.
▧ Metabolism :
Metabolism is limited (<10%). Most of the active compound is excreted renally (81%). A small proportion is glucuronidated, oxidated, N-formylated or conjugated to a hexose.
▧ Route of Elimination :
Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2.
▧ Half Life :
The elimination half-life of varenicline is approximately 24 hours
Chỉ Định : For use as an aid in smoking cessation.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Champix
  • Công ty :
    Sản phẩm biệt dược : Chantix
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01273
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5310966
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505502
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470510.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0069-0471-97
PharmGKB
http://www.pharmgkb.org/drug/PA164781343
Wikipedia
http://en.wikipedia.org/wiki/Varenicline
RxList
http://www.rxlist.com/cgi/generic/chantix.htm
Drugs.com
http://www.drugs.com/cdi/varenicline.html
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