Tìm theo
Methylscopolamine bromide
Các tên gọi khác (10 ) :
  • (−)-scopolamine methobromide
  • (−)-scopolamine methyl bromide
  • Hyoscine Methobromide
  • Hyoscine methyl bromide
  • Methscopolamine bromide
  • N-methylhyoscine bromide
  • N-methylscopolammonium bromide
  • Pamine
  • Scopolamine Methobromide
  • Scopolamine methyl bromide
parasympatholytics, cholinergic antagonists, antispasmodics
Thuốc Gốc
Small Molecule
CAS: 155-41-9
ATC: A03BB03, S01FA03
ĐG : A. Aarons Inc. , http://www.aaronindustriesinc.com
CTHH: C18H24BrNO4
PTK: 398.291
A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H24BrNO4
Phân tử khối
398.291
Monoisotopic mass
397.088870908
InChI
InChI=1S/C18H24NO4.BrH/c1-19(2)14-8-12(9-15(19)17-16(14)23-17)22-18(21)13(10-20)11-6-4-3-5-7-11;/h3-7,12-17,20H,8-10H2,1-2H3;1H/q+1;/p-1/t12?,13-,14+,15+,16?,17?;/m1./s1
InChI Key
InChIKey=CXYRUNPLKGGUJF-JIRGPDKYSA-M
IUPAC Name
(1S,5S,7R)-7-{[(2S)-3-hydroxy-2-phenylpropanoyl]oxy}-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0^{2,4}]nonan-9-ium bromide
Traditional IUPAC Name
(1S,5S,7R)-7-{[(2S)-3-hydroxy-2-phenylpropanoyl]oxy}-9,9-dimethyl-3-oxa-9-azatricyclo[3.3.1.0^{2,4}]nonan-9-ium bromide
SMILES
[Br-].[H][C@]12C[C@@H](C[C@@]([H])(C3OC13)[N+]2(C)C)OC(=O)[C@H](CO)C1=CC=CC=C1
Độ tan chảy
225 °C
Độ hòa tan
Freely soluble
logP
-2.58
logS
-4.5
pKa (strongest acidic)
15.15
pKa (Strongest Basic)
-2.7
PSA
55.76 Å2
Refractivity
95.63 m3·mol-1
Polarizability
48.12 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
caco2 Permeability
-6.16
Dược Lực Học : Methscopolamine is a muscarinic antagonist structurally similar to the neurotransmitter acetylcholine and acts by blocking the muscarinic acetylcholine receptors and is thus classified as an anticholinergic. Methscopolamine has many uses including the prevention of motion sickness. It is not clear how Methscopolamine prevents nausea and vomiting due to motion sickness. The vestibular part of the ear is very important for balance. When a person becomes disoriented due to motion, the vestibule sends a signal through nerves to the vomiting center in the brain, and vomiting occurs. Acetylcholine is a chemical that nerves use to transmit messages to each other. It is believe that Methscopolamine prevents communication between the nerves of the vestibule and the vomiting center in the brain by blocking the action of acetylcholine. Methscopolamine also may work directly on the vomiting center. Methscopolamine must be taken before the onset of motion sickness to be effective.
Cơ Chế Tác Dụng : A muscarinic antagonist used to study binding characteristics of muscarinic cholinergic receptors. [PubChem] Methscopolamine acts by interfering with the transmission of nerve impulses by acetylcholine in the parasympathetic nervous system (specifically the vomiting center). It does so by acting as a muscarinic antagonist.
Dược Động Học :
▧ Absorption :
Poorly and unreliably absorbed, total absorption is 10-25%.
▧ Metabolism :
Little is known about the fate and excretion of methscopolamine.
Độc Tính : Symptoms of a methscopolamine overdose include headache, nausea, vomiting, dry mouth, difficulty swallowing, blurred vision, dilated pupils, hot, dry skin, dizziness; drowsiness, confusion, anxiety, seizures, weak pulse, and an irregular heartbeat. In addition, a curare-like action may occur, i.e., neuromuscular blockade leading to muscular weakness and possible paralysis.
Chỉ Định : Used as adjunctive therapy for the treatment of peptic ulcer. Also used to treat nausea and vomiting due to motion sickness.
Tương Tác Thuốc :
  • Cinitapride Anticholinergic agents like methylscopolamine may reduce the action of cinitapride.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Methylscopolamine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Trimethobenzamide Trimethobenzamide and Methylscopolamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Methylscopolamine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trospium Trospium and Methylscopolamine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Methscopolamine
  • Công ty :
    Sản phẩm biệt dược : Pamine
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00462
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=23724781
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506260
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00715
ChemSpider
http://www.chemspider.com/Chemical-Structure.3977.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/60429-251
PharmGKB
http://www.pharmgkb.org/drug/PA164784032
Wikipedia
http://en.wikipedia.org/wiki/Methylscopolamine
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