Tìm theo
Buclizine
Các tên gọi khác (4 ) :
  • 1-(P-Tert-butylbenzyl)-4-(4-chloro-alpha-phenylbenzyl)piperazine
  • Buclizina
  • Buclizine
  • Buclizinum
cholinergic antagonists, histamine antagonists
Thuốc Gốc
Small Molecule
CAS: 82-95-1
ATC: R06AE01
CTHH: C28H33ClN2
PTK: 433.028
Buclizine is an antihistamine of the piperazine derivative family. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C28H33ClN2
Phân tử khối
433.028
Monoisotopic mass
432.233226773
InChI
InChI=1S/C28H33ClN2/c1-28(2,3)25-13-9-22(10-14-25)21-30-17-19-31(20-18-30)27(23-7-5-4-6-8-23)24-11-15-26(29)16-12-24/h4-16,27H,17-21H2,1-3H3
InChI Key
InChIKey=MOYGZHXDRJNJEP-UHFFFAOYSA-N
IUPAC Name
1-[(4-tert-butylphenyl)methyl]-4-[(4-chlorophenyl)(phenyl)methyl]piperazine
Traditional IUPAC Name
buclizine
SMILES
CC(C)(C)C1=CC=C(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)C=C1
Độ sôi
218 °C
Độ hòa tan
2.46e-04 g/l
logP
7.1
logS
-6.2
pKa (Strongest Basic)
8.04
PSA
6.48 Å2
Refractivity
133.02 m3·mol-1
Polarizability
50.93 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 : Buclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Buclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which buclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects.
Cơ Chế Tác Dụng : Buclizine is an antihistamine of the piperazine derivative family. [Wikipedia] Vomiting (emesis) is essentially a protective mechanism for removing irritant or otherwise harmful substances from the upper GI tract. Emesis or vomiting is controlled by the vomiting centre in the medulla region of the brain, an important part of which is the chemotrigger zone (CTZ). The vomiting centre possesses neurons which are rich in muscarinic cholinergic and histamine containing synapses. These types of neurons are especially involved in transmission from the vestibular apparatus to the vomiting centre. Motion sickness principally involves overstimulation of these pathways due to various sensory stimuli. Hence the action of buclizine which acts to block the histamine receptors in the vomiting centre and thus reduce activity along these pathways. Furthermore since buclizine possesses anti-cholinergic properties as well, the muscarinic receptors are similarly blocked.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration.
▧ Metabolism :
Hepatic.
Chỉ Định : For prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems).
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Bucladin
  • Công ty :
    Sản phẩm biệt dược : Bucladin-S
  • Công ty : Novartis India
    Sản phẩm biệt dược : Longifene Syrup
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00354
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6729
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507608
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07777
ChemSpider
http://www.chemspider.com/Chemical-Structure.6473.html
PharmGKB
http://www.pharmgkb.org/drug/PA164748223
Wikipedia
http://en.wikipedia.org/wiki/Buclizine
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