Tìm theo
Methysergide
Các tên gọi khác (12 ) :
  • (+)-9,10-Didehydro-N-(1-(hydroxymethyl)propyl)-1,6-dimethylergoline-8beta-carboxamide
  • (+)-N-(1-(Hydroxymethyl)propyl)-1-methyl-D-lysergamide
  • 1-Methyl-D-lysergic acid butanolamide
  • 1-Methyl-dextro-lysergic acid (+)-1-hydroxy-2-butylamide
  • 1-Methyllysergic acid butanolamide
  • 1-Methylmethylergonovine
  • 9,10-Didehydro-N-(1-(hydroxymethyl)propyl)-1,6-dimethylergoline-8-carboxamide
  • Methysergide
  • Methysergidum
  • Metisergida
  • Metisergido
  • N-(1-(Hydroxymethyl)propyl)-1-methyl-dextro-(+)-lysergamide
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 361-37-5
ATC: N02CA04
ĐG : Novartis AG , http://www.novartis.com
CTHH: C21H27N3O2
PTK: 353.458
An ergot derivative that is a congener of lysergic acid diethylamide. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H27N3O2
Phân tử khối
353.458
Monoisotopic mass
353.210327123
InChI
InChI=1S/C21H27N3O2/c1-4-15(12-25)22-21(26)14-8-17-16-6-5-7-18-20(16)13(10-23(18)2)9-19(17)24(3)11-14/h5-8,10,14-15,19,25H,4,9,11-12H2,1-3H3,(H,22,26)/t14-,15?,19-/m1/s1
InChI Key
InChIKey=KPJZHOPZRAFDTN-NQUBZZJWSA-N
IUPAC Name
(4R,7R)-N-(1-hydroxybutan-2-yl)-6,11-dimethyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide
Traditional IUPAC Name
(4R,7R)-N-(1-hydroxybutan-2-yl)-6,11-dimethyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(16),2,9,12,14-pentaene-4-carboxamide
SMILES
[H][C@@]12CC3=CN(C)C4=C3C(=CC=C4)C1=C[C@H](CN2C)C(=O)NC(CC)CO
Độ tan chảy
195 °C
Độ hòa tan
2.24e-01 g/l
logP
1.5
logS
-3.2
pKa (strongest acidic)
15.01
pKa (Strongest Basic)
7.85
PSA
57.5 Å2
Refractivity
104.47 m3·mol-1
Polarizability
40.41 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Methysergide has been shown, in vitro and in vivo, to inhibit or block the effects of serotonin, a substance which may be involved in the mechanism of vascular headaches. Serotonin has been variously described as a central neurohumoral agent or chemical mediator, as a "headache substance" acting directly or indirectly to lower pain threshold, as an intrinsic "motor hormone" of the gastrointestinal tract, and as a "hormone" involved in connective tissue reparative processes.
Cơ Chế Tác Dụng : An ergot derivative that is a congener of lysergic acid diethylamide. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome. [PubChem] Methysergide is serotonin antagonists acts on central nervous system (CNS), which directly stimulates the smooth muscle leading to vasoconstriction. Some alpha-adrenergic blocking activity has been reported. Suggestions have been made by investigators as to the mechanism whereby Methysergide produces its clinical effects, but this has not been finally established, although it may be related to the antiserotonin effect.
Dược Động Học :
▧ Absorption :
Rapid
▧ Metabolism :
Hepatic
Độc Tính : Few cases of acute methysergide intoxication have been reported. The possible symptom complex is therefore not fully known. The following symptoms are based on these few case reports. Euphoria, hyperactivity, tachycardia, dilated pupils, and dizziness have been reported in a child with a dose of 20-24 mg of methysergide. In adults, peripheral vasospasm, with diminished or absent pulses, coldness, mottling and cyanosis, has been observed at a dose of 200 mg. Ischemic tissue damage has not been reported in acute overdosage with methysergide.
Chỉ Định : For the treatment of vascular headache
Tương Tác Thuốc :
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Deseril
  • Công ty :
    Sản phẩm biệt dược : Desernil
  • Công ty :
    Sản phẩm biệt dược : Sansert
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00247
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07199
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02357
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50031942
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0078-0058-05
PharmGKB
http://www.pharmgkb.org/drug/PA164743265
Wikipedia
http://en.wikipedia.org/wiki/Methysergide
RxList
http://www.rxlist.com/cgi/generic3/sansert.htm
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