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萝巴新

萝巴新用途

盐酸阿马利辛(劳巴辛)是一种有效的肾上腺素能溶解剂,优先阻断α1-肾上腺素受体。盐酸阿马利辛是一种可逆但非竞争性的尼古丁受体全抑制剂,IC50为72.3μM。盐酸阿马利辛也可用作抗高血压药和蛇纹石,具有镇静作用[1][2]。

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萝巴新名称

[ CAS 号 ]:
4373-34-6

[ 中文名 ]:
萝巴新

[ 英文名 ]:
Ajmalicine hydrochloride

[中文别名 ]:

盐酸阿吗碱

[英文别名 ]:

Circolene
Pytetrahydroserpentine
Einecs 224-471-9
d-Yohimbine
δ-Yohimbine
RAUBASINE HYDROCHLORIDE
AJMALICINE HCL
Raubasine
Ajmalicine
ajmalicine,monohydrochloride

萝巴新生物活性

[ 描述 ]:

[ 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 >> 肾上腺素能受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> 疼痛

[ 靶点 ]

α1-adrenergic receptor

α2-adrenergic receptor

[体外研究]

盐酸阿马利辛优先阻断α1-肾上腺素受体,而不是α2-肾上腺素受体[1]。盐酸阿马利辛以浓度依赖性方式抑制收缩(IC50=72.3±22.5μM)[2]。盐酸阿马利辛优先作用于突触后位点,以pA2值6.57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,以PA1值6.2阻断可乐定的抑制作用[3]。

[体内研究]

盐酸阿马利辛可阻断电刺激的升压作用,并对交感神经刺激有效[1]。盐酸阿马利辛(0.5-4 mg/kg)对去甲肾上腺素的升压反应产生明显的剂量依赖性抑制[1]。动物模型：雄性Wistar大鼠(300-350 g)[1]剂量：0.5、1、2和4 mg/kg给药：静脉注射,一次结果：诱导对去甲肾上腺素升压反应的显著剂量依赖性抑制。

[参考文献]

[1]. 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.

[2]. 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.

[3]. 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 ]:
275-300ºC

[ 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、食品添加剂分开存放

萝巴新毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AX7890000

CHEMICAL NAME :: Ajmalicine, hydrochloride

CAS REGISTRY NUMBER :: 4373-34-6

LAST UPDATED :: 199306

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C21-H24-N2-O3.Cl-H

MOLECULAR WEIGHT :: 388.93

WISWESSER LINE NOTATION :: T F6 D5 C666 EM ON SO TU&&TTTJ R1 UVO1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: LDBU** "Zur Pharmakologie der Yohimbealkaloide, Dissertation," Langer, J., Institute fuer Pharmakologie und Experimentelle Therapie der Universitat Breslau, Poland, 1932 Volume(issue)/page/year: -,-,1932

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 56 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: CSLNX* U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals. (Aberdeen Proving Ground, MD 21010) Volume(issue)/page/year: NX#00444

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萝巴新安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ WGK德国 ]:
3

[ RTECS号 ]:
AX7890000

萝巴新