Naloxonazine dihydrochloride

• 常用名: Naloxonazine dihydrochloride
• 英文名: Naloxonazine dihydrochloride
• CAS号: 880759-65-9
• 分子量: 687.22400
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₈H₄₃ClN₄O₆
• 熔点: N/A
• 闪点: N/A

Naloxonazine dihydrochloride用途

盐酸纳络嗪是一种特异性μ-阿片受体拮抗剂,IC50为5.4 nM。盐酸纳络嗪也具有抗利什曼病活性[1][2][3]。

Naloxonazine dihydrochloride名称

• 英文名: Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-, [(5α)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene]hydrazone, dihydrochloride, (5α)

Naloxonazine dihydrochloride生物活性

• 描述: 盐酸纳络嗪是一种特异性μ-阿片受体拮抗剂,IC50为5.4 nM。盐酸纳络嗪也具有抗利什曼病活性[1][2][3]。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体
  信号通路 >> 神经信号通路 >> 阿片受体
  研究领域 >> 神经疾病
• 靶点实验:

  μ-opioid receptor:5.4 nM (IC50)

• 体外研究: 纳络嗪在溶液中相对稳定[2]。纳络嗪(72小时)对杜氏利什曼原虫的细胞内无鞭毛期具有活性,其半数最大抑制浓度(GI50)为3.45μM[3]。纳洛酮嗪(10μM；0-72小时)在杜氏利什曼原虫感染的早期阶段具有活性[3]。纳络嗪影响宿主细胞的酸性隔室,进而限制杜氏乳杆菌的细胞内生长[3]。
• 体内研究: 纳络嗪(20 mg/kg；i.p.；1次)可减弱急性甲基苯丙胺诱导小鼠运动活性的增加[1]动物模型：雄性ICR小鼠,甲基苯乙胺(METH)诱导的运动活性模型[1]剂量：20 mg/kg给药：腹腔注射,1次,在注射生理盐水(i.p.)或METH(1 mg/kg,i.p。
• 参考文献:

  [1]. Chien CC, et al. Naloxonazine, a specific mu-opioid receptor antagonist, attenuates the increment of locomotor activity induced by acute methamphetamine in mice. Toxicol Lett. 2012 Jul 7;212(1):61-5.

  [2]. Hahn EF, et al. Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites. Life Sci. 1982 Sep 20-27;31(12-13):1385-8.

  [3]. De Muylder G, et al. Naloxonazine, an Amastigote-Specific Compound, Affects Leishmania Parasites through Modulation of Host-Encoded Functions. PLoS Negl Trop Dis. 2016 Dec 30;10(12):e0005234.

Naloxonazine dihydrochloride物理化学性质

• 分子式: C₃₈H₄₃ClN₄O₆
• 分子量: 687.22400
• 精确质量: 686.28700
• PSA: 130.58000
• LogP: 3.95300
• InChIKey: VIAIHLLKDJKEKM-UHFFFAOYSA-N
• SMILES: C=CCN1CCC23c4c5ccc(O)c4OC2C(=NN=C2CCC4(O)C6Cc7ccc(O)c8c7C4(CCN6CC=C)C2O8)CCC3(O)C1C5.Cl.Cl

Naloxonazine dihydrochloride靶点实验

查看更多实验

实验名称：qHTS for Inhibitors of Polymerase Iota 来源：NCGC 靶标：DNA polymerase iota [Homo sapiens] External Id：PolI100

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实验名称：qHTS Assay for Small Molecule Inhibitors of the Human hERG Channel Activity 来源：NCGC External Id：HERG01

实验名称：qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1):... 来源：NCGC 靶标：thioredoxin reductase [Rattus norvegicus] External Id：TRXR100

实验名称：Cell-based high throughput primary assay to identify activators of GPR151 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=G-protein coupled receptor 151; AltName: Full=G-protein coupled receptor PGR7; AltName: Full=GPCR-2037; AltName: Full=Galanin receptor 4; AltName: Full=Galanin-receptor-like protein; Short=GalRL External Id：GPR151_PHUNTER_AG_LUMI_1536_1X%ACT

实验名称：Quantitative high throughput screen for delayed death inhibitors of the malarial para... 来源：NCGC 靶标：N/A External Id：DDV296

实验名称：LOPAC HTS for Inhibitors of Aerobactin Synthetase IucA 来源：23265 靶标：IucA from hypervirulent Klebsiella pneumoniae External Id：IucA Pilot Assay LOPAC Library

实验名称：96-well format Chlamydomonas reinhardtii Algae Gravitaxis Assay to measure the differ... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：N/A External Id：MH081217, Chlamydomonas reinhardtii Gravitaxis Assay to Identify Small Molecule Inhibitors of Cilia.

实验名称：Quantitative high throughput screen for delayed death inhibitors of the malarial para... 来源：NCGC 靶标：N/A External Id：DDV248

实验名称：AlphaScreen-based biochemical high throughput primary assay to identify activators of... 来源：The Scripps Research Institute Molecular Screening Center 靶标：N/A External Id：FBW7_ACT_ALPHA_1536_1X%ACT PRUN

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Naloxonazine dihydrochloride英文别名

• NALOXONAZINE DIHYDROCHLORIDE HYDRATE
• NALOXONAZINE DIHYDROCHLORIDE OPIOID ANTA GONIST
• Naloxonazine dihydrochloride
• Demethylasterriquinone B1