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萝巴新; 阿吗碱

萝巴新; 阿吗碱用途

Ajmalicine (Raubasine) 阿吗里新,长春花草药中发现,是一种降压药,用于治疗高血压,降低外周阻力和血压。Ajmalicine (Raubasine) 是一种肾上腺素能药物,优先阻断 α1-肾上腺素受体 alpha 1-adrenoceptor。Ajmalicine (Raubasine) 是一种可逆的非竞争性尼古丁受体拮抗剂 (IC50=72.3 μM)。Ajmalicine (Raubasine) 优先作用于突触后部位,竞争性拮抗去甲肾上腺素对突触后 α 肾上腺素受体的作用 (pA2=6.57), 竞争性阻断可乐定的抑制作用 (pA2=6.2)。

萝巴新; 阿吗碱名称

[ CAS 号 ]:
483-04-5

[ 中文名 ]:
萝巴新

[ 英文名 ]:
Ajmalicine

[中文别名 ]:

[英文别名 ]:

萝巴新; 阿吗碱生物活性

[ 描述 ]:

Ajmalicine (Raubasine) 阿吗里新,长春花草药中发现,是一种降压药,用于治疗高血压,降低外周阻力和血压。Ajmalicine (Raubasine) 是一种肾上腺素能药物,优先阻断 α1-肾上腺素受体 alpha 1-adrenoceptor。Ajmalicine (Raubasine) 是一种可逆的非竞争性尼古丁受体拮抗剂 (IC50=72.3 μM)。Ajmalicine (Raubasine) 优先作用于突触后部位,竞争性拮抗去甲肾上腺素对突触后 α 肾上腺素受体的作用 (pA2=6.57), 竞争性阻断可乐定的抑制作用 (pA2=6.2)。

[ 相关类别 ]:

研究领域 >> 心血管疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
信号通路 >> 神经信号通路 >> 疼痛

[参考文献]

[1]. Wink, Michael; Roberts, M. W. (1998). Alkaloids: biochemistry, ecology, and medicinal applications. New York: Plenum Press. ISBN 0-306-45465-3.

[2]. Roquebert J, et al. Inhibition of the alpha 1 and alpha 2-adrenoceptor-mediated pressor response in pithed rats by raubasine, tetrahydroalstonine and akuammigine. Eur J Pharmacol. 1984 Oct 30;106(1):203-5.

[3]. Pereira DM, et al. Pharmacological effects of Catharanthus roseus root alkaloids in acetylcholinesterase inhibition and cholinergic neurotransmission. Phytomedicine. 2010 Jul;17(8-9):646-52.

[4]. • Demichel P, et al. Effects of raubasine stereoisomers on pre- and postsynaptic alpha-adrenoceptors in the rat vas deferens. Br J Pharmacol. 1984 Oct;83(2):505-10

萝巴新; 阿吗碱物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
524.0±50.0 °C at 760 mmHg

[ 熔点 ]:
258°C (rough estimate)

[ 分子式 ]:
C21H24N2O3

[ 分子量 ]:
352.427

[ 闪点 ]:
270.7±30.1 °C

[ 精确质量 ]:
352.178680

[ PSA ]:
54.56000

[ LogP ]:
2.88

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.656

[ 储存条件 ]:
库房通风低温干燥,与氧化剂、酸类、食品添加剂分开存放

萝巴新; 阿吗碱MSDS

萝巴新; 阿吗碱毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AX7875000
CHEMICAL NAME :
Ajmalicine
CAS REGISTRY NUMBER :
483-04-5
BEILSTEIN REFERENCE NO. :
0097268
LAST UPDATED :
199612
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C21-H24-N2-O3
MOLECULAR WEIGHT :
352.47
WISWESSER LINE NOTATION :
T F6 D5 C666 EM ON SO TU&&TTTJ R1 UVO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - child
DOSE/DURATION :
12500 ug/kg
TOXIC EFFECTS :
Behavioral - general anesthetic Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes
REFERENCE :
CHETBF Chest. (American College of Chest Physicians, 911 Busse Hwy, Park Ridge, IL 60068) V.57- 1970- Volume(issue)/page/year: 76,97,1979
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
750 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 233,72,1958
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
200 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: -,117,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
24 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: -,117,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
400 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: -,117,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
165 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: -,117,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 233,72,1958
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
500 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: -,117,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
20 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: -,117,1972
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
20 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 23,600,1973

萝巴新; 阿吗碱安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R25

[ 安全声明 (欧洲) ]:
22-45

[ 危险品运输编码 ]:
UN 1544

[ RTECS号 ]:
AX7875000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

萝巴新; 阿吗碱上下游产品

萝巴新; 阿吗碱上游产品

萝巴新; 阿吗碱下游产品

萝巴新; 阿吗碱文献

Determination of terpenoid indole alkaloids in hairy roots of Rhazya stricta (Apocynaceae) by GC-MS.

Phytochem. Anal. 26 , 331-8, (2015)

Rhazya stricta Decne. (Apocynaceae) is a medicinal plant rich in terpenoid indole alkaloids (TIAs), some of which possess important pharmacological properties. The study material including transgenic ...

Synergistic and cytotoxic action of indole alkaloids produced from elicited cell cultures of Catharanthus roseus.

Pharm. Biol. 51(3) , 304-10, (2013)

Catharanthus roseus (L.) G. Don (Apocynaceae) is a medicinal plant that produces more than 130 alkaloids, with special attention given to the production of the anti-hypertensive monomeric indole alkal...

A differential response to chemical elicitors in Catharanthus roseus in vitro cultures.

Biotechnol. Lett. 31(4) , 591-5, (2009)

The effects of methyl jasmonate, salicylic acid and ethylene on alkaloid accumulation in in vitro cell suspension, hairy roots and rootless shoot cultures of Catharanthus roseus were analyzed. Ajmalic...


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¥389.0/5mg ¥1649.0/25mg ¥700.0/10mg ¥需询单/1g

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产品详情:[Perfemiker]阿马碱,≥98%(HPLC)


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