萝巴新

• 常用名: 萝巴新
• 英文名: Ajmalicine hydrochloride
• CAS号: 4373-34-6
• 分子量: 352.427
• 密度: 1.3±0.1 g/cm3
• 沸点: 524.0±50.0 °C at 760 mmHg
• 分子式: C₂₁H₂₄N₂O₃
• 熔点: 275-300ºC
• 闪点: 270.7±30.1 °C

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]。

萝巴新名称

• 中文名: 萝巴新
• 英文名: ajmalicine hydrochloride
• 中文别名: 盐酸阿吗碱

萝巴新生物活性

• 描述: 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]。
• 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
• 靶点实验:

  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
• InChIKey: YWPZOTNKHMBWPD-QAWKRFFXSA-N
• SMILES: COC(=O)C1=COC(C)C2CN3CCc4c([nH]c5ccccc45)C3CC12.Cl
• 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

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

萝巴新靶点实验

查看更多实验

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实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

实验名称：Absorbance-based primary biochemical high throughput screening assay to identify acti... 来源：The Scripps Research Institute Molecular Screening Center 靶标：caspase-3 preproprotein [Homo sapiens] External Id：PROCASPASE3_ACT_EPIABS_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule modulators of NR3A 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：SBCCG-A1015-NR3A-Primary-Assay

实验名称：uHTS identification of small molecule modulators of Rev-erb Alpha. 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：SBCCG-A1016-RevErbaLBD-Primary-Assay

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萝巴新英文别名

• Circolene
• Pytetrahydroserpentine
• Einecs 224-471-9
• d-Yohimbine
• δ-Yohimbine
• RAUBASINE HYDROCHLORIDE
• AJMALICINE HCL
• (19α)-16,17-Didehydro-19-methyl-oxayohimban-16-carboxylic acid methyl ester
• Methyl (19α)-19-methyl-16,17-didehydro-18-oxayohimban-16-carboxylate
• Methyl (4S,4aR,13bS,14aS)-4-methyl-4a,5,7,8,13,13b,14,14a-octahydro-4H-indolo[2,3-a]pyrano[3,4-g]quinolizine-1-carboxylate
• Raubasine
• Ajmalicine
• ajmalicine,monohydrochloride
• Lamuran
• Methyl-(4S,4aR,13bS,14aS)-4-methyl-4a,5,7,8,13,13b,14,14a-octahydro-4H-indolo[2,3-a]pyrano[3,4-g]chinolizin-1-carboxylat
• Methyl-(19α)-19-methyl-16,17-didehydro-18-oxayohimban-16-carboxylat
• AJMALICIN HCL
• Tetrahydroserpentine