Tìm theo
Azatadine
Các tên gọi khác (7 ) :
  • 11-(1-Methyl-4-piperidinylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
  • 6,11-Dihydro-11-(1-methyl-4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine
  • Azatadin
  • Azatadina
  • Azatadine
  • Azatadine Maleate
  • Azatadinum
histamine h1 antagonists
Thuốc Gốc
Small Molecule
CAS: 3964-81-6
ATC: R06AX09
CTHH: C20H22N2
PTK: 290.4021
Antihistamines such as azatadine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H22N2
Phân tử khối
290.4021
Monoisotopic mass
290.178298714
InChI
InChI=1S/C20H22N2/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19/h2-7,12H,8-11,13-14H2,1H3
InChI Key
InChIKey=SEBMTIQKRHYNIT-UHFFFAOYSA-N
IUPAC Name
2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaene
Traditional IUPAC Name
2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaene
SMILES
CN1CCC(CC1)=C1C2=CC=CC=C2CCC2=C1N=CC=C2
Độ tan chảy
152-154
Độ hòa tan
Very soluble
logP
3.59
logS
-3.4
pKa (Strongest Basic)
7.91
PSA
16.13 Å2
Refractivity
101.53 m3·mol-1
Polarizability
34.01 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Azatadine is an antihistamine, related to cyproheptadine, with anti-serotonin, anticholinergic (drying), and sedative effects. Azatadine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, azatadine is not used clinically as an anti-psychotic. Antihistamines antagonize the vasodilator effect of endogenously released histamine, especially in small vessels, and mitigate the effect of histamine which results in increased capillary permeability and edema formation. As consequences of these actions, antihistamines antagonize the physiological manifestations of histamine release in the nose following antigen-antibody interaction, such as congestion related to vascular engorgement, mucosal edema, and profuse, watery secretion, and irritation and sneezing resulting from histamine action on afferent nerve terminals.
Cơ Chế Tác Dụng : Antihistamines such as azatadine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release. Antihistamines such as azatadine appear to compete with histamine for histamine H1- receptor sites on effector cells. The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Dược Động Học :
▧ Absorption :
Well absorbed after oral administration.
▧ Metabolism :
Hepatic.
Độc Tính : The oral LD50 in mature rats and mice was greater than 1700 mg/kg and 600 mg/kg, respectively. Symptoms of overdose include clumsiness or unsteadiness, seizures, severe drowsiness, flushing or redness of face, hallucinations, muscle spasms (especially of neck and back), restlessness, shortness of breath, shuffling walk, tic-like (jerky) movements of head and face, trembling and shaking of hands, and insomnia.
Chỉ Định : For the relief of the symptoms of upper respiratory mucosal congestion in perennial and allergic rhinitis, and for the relief of nasal congestion and eustachian t.b. congestion.
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : NIHFI
    Sản phẩm biệt dược : Idumed
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Optimine
  • Công ty : Fulford
    Sản phẩm biệt dược : Zadine
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00719
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=19861
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507958
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07774
ChemSpider
http://www.chemspider.com/Chemical-Structure.18709.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22868
PharmGKB
http://www.pharmgkb.org/drug/PA164747157
Wikipedia
http://en.wikipedia.org/wiki/Azatadine
RxList
http://www.rxlist.com/cgi/generic3/azatpseud.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/tri1460.shtml
Drugs.com
http://www.drugs.com/mtm/azatadine.html
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