甲麦角新碱

甲麦角新碱用途

甲基麦角新碱(甲基麦角新碱)是一种口服活性5-HT2B配体激动剂。甲基麦角新碱可用作催产素,对产后出血有保护作用[1][2][3]。

甲麦角新碱名称

[ CAS 号 ]:
113-42-8

[ 中文名 ]:
甲麦角新碱

[ 英文名 ]:
Methylergometrine

[英文别名 ]:

甲麦角新碱生物活性

[ 描述 ]:

甲基麦角新碱(甲基麦角新碱)是一种口服活性5-HT2B配体激动剂。甲基麦角新碱可用作催产素,对产后出血有保护作用[1][2][3]。

[ 相关类别 ]:

研究领域 >> 内分泌
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

5-HT2B Receptor


[参考文献]

[1]. Hajjo R, et al. Development, validation, and use of quantitative structure-activity relationship models of 5-hydroxytryptamine (2B) receptor ligands to identify novel receptor binders and putative valvulopathic compounds among common drugs. J Med Chem. 2010 Nov 11;53(21):7573-86.  

[2]. Svanström MC, et al. Signs of myocardial ischaemia after injection of oxytocin: a randomized double-blind comparison of oxytocin and methylergometrine during Caesarean section. Br J Anaesth. 2008 May;100(5):683-9.  

[3]. Amant F, et al. Misoprostol compared with methylergometrine for the prevention of postpartum haemorrhage: a double-blind randomised trial. Br J Obstet Gynaecol. 1999 Oct;106(10):1066-70.  

甲麦角新碱物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
638.4±55.0 °C at 760 mmHg

[ 熔点 ]:
172ºC

[ 分子式 ]:
C20H25N3O2

[ 分子量 ]:
339.431

[ 闪点 ]:
339.9±31.5 °C

[ 精确质量 ]:
339.194672

[ PSA ]:
68.36000

[ LogP ]:
1.67

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.665

甲麦角新碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KE5425000
CHEMICAL NAME :
Ergoline-8-beta-carboxamide, 9,10-didehydro-N-((S)-1-(hydroxymethyl)propyl)-6-meth yl-
CAS REGISTRY NUMBER :
113-42-8
LAST UPDATED :
199509
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C20-H25-N3-O2
MOLECULAR WEIGHT :
339.48
WISWESSER LINE NOTATION :
T C6656 1A P GN LM CUTT&&J EVMY2&1Q G1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
93 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,163,1973
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
23 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,100,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
187 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,163,1973
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
85 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,163,1973
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
64 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
PLRCAT Pharmacological Research Communications. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1969- Volume(issue)/page/year: 9,299,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
2600 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,163,1973 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
10 mg/kg
SEX/DURATION :
female 12-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
AJPHAP American Journal of Physiology. (American Physiological Soc., 9650 Rockville Pike, Bethesda, MD 20814) V.1- 1898- Volume(issue)/page/year: 180,296,1955 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4271 No. of Facilities: 17 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 295 (estimated) No. of Female Employees: 243 (estimated)

甲麦角新碱合成路线

详细合成路线

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