Tìm theo
Cinnarizine
Các tên gọi khác (8 ) :
  • 1-(Diphenylmethyl)-4-(3-phenyl-2-propenyl)piperazine
  • 1-Benzhydryl-4-cinnamylpiperazin
  • 1-Cinnamyl-4-(diphenylmethyl)piperazine
  • Cinarizina
  • Cinnarizin
  • Cinarizin
  • Cinnarizine
  • Cinnarizinum
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 298-57-7
ATC: N07CA02
CTHH: C26H28N2
PTK: 368.5139
Cinnarizine is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception. Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination each drug potentiate the other in boosting brain oxygen supply.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H28N2
Phân tử khối
368.5139
Monoisotopic mass
368.225248906
InChI
InChI=1S/C26H28N2/c1-4-11-23(12-5-1)13-10-18-27-19-21-28(22-20-27)26(24-14-6-2-7-15-24)25-16-8-3-9-17-25/h1-17,26H,18-22H2/b13-10+
InChI Key
InChIKey=DERZBLKQOCDDDZ-JLHYYAGUSA-N
IUPAC Name
1-(diphenylmethyl)-4-(3-phenylprop-2-en-1-yl)piperazine
Traditional IUPAC Name
1-(diphenylmethyl)-4-(3-phenylprop-2-en-1-yl)piperazine
SMILES
C(C=CC1=CC=CC=C1)N1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1
Độ hòa tan
750 mg/L (at 25 °C)
logP
5.77
logS
-5.3
pKa (Strongest Basic)
8.4
PSA
6.48 Å2
Refractivity
119.86 m3·mol-1
Polarizability
43.96 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.
Cơ Chế Tác Dụng : Cinnarizine is an anti-histaminic drug which is mainly used for the control of vomiting due to motion sickness. Cinnarizine was first synthesized by Janssen Pharmaceutica in 1955. It acts by interfering with the signal transmission between vestibular apparatus of the inner ear and the vomiting centre of the hypothalamus. The disparity of signal processing between inner ear motion receptors and the visual senses is abolished, so that the confusion of brain whether the individual is moving or standing is reduced. Vomiting in motion sickness is actually a physiological compensatory mechanism of the brain to keep the individual from moving so that it can adjust to the signal perception. Cinnarizine could be also viewed as a nootropic drug because of its vasorelaxating abilities (due to calcium channel blockage), which happen mostly in brain. It is also effectively combined with other nootropics, primarily piracetam; in such combination each drug potentiate the other in boosting brain oxygen supply. Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.
Chỉ Định : For the treatment of vertigo/meniere's disease, nausea and vomiting, motion sickness and also useful for vestibular symptoms of other origins.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Italchimici
    Sản phẩm biệt dược : Cinazyn
  • Công ty : Streuli Pharma
    Sản phẩm biệt dược : Cinnageron
  • Công ty : Ivax
    Sản phẩm biệt dược : Folcodal
  • Công ty : Janssen-Cilag
    Sản phẩm biệt dược : Sepan
  • Công ty : Janssen
    Sản phẩm biệt dược : Stugeron
  • Công ty : Janssen
    Sản phẩm biệt dược : Stugeron Forte
  • Công ty : Scharper
    Sản phẩm biệt dược : Toliman
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00568
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=1547484
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506769
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01295
ChemSpider
http://www.chemspider.com/Chemical-Structure.2659.html
PharmGKB
http://www.pharmgkb.org/drug/PA164749342
Wikipedia
http://en.wikipedia.org/wiki/Cinnarizine
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