Luminol sodium salt | 20666-12-0

• 物质功能分类: 生物 - 细胞培养 - 添加剂
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Luminol sodium salt
• CAS: 20666-12-0
• 化学式: C8H7N3NaO2
• 分子量: 200.15
• InChiKey: JKEBMURXLKGPLR-UHFFFAOYSA-N

物化性质

• 熔点：
  319-320 C

计算性质

• 辛醇/水分配系数(LogP)：
  -0.58
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  84.2
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S26,S36
• 危险类别码：
  R36/37/38
• WGK Germany：
  3
• 海关编码：
  2933990090
• 危险标志：
  GHS07
• 危险性描述：
  H315,H319,H335
• 危险性防范说明：
  P261,P305 + P351 + P338

制备方法与用途

RP底物：鲁米诺

鲁米诺（3-氨基邻苯二甲酰肼）是最早使用、应用最广泛且量子产率较高的化学发光试剂之一。自1928年Albrecht首次报道了鲁米诺与氧化剂在碱性溶液中的化学发光行为以来，该化学发光反应主要用于测定氧化剂与无机金属离子。近年来，研究人员不仅进一步研究了这一化学发光反应，还将它与其他多种分析技术结合使用，使得其应用范围不断扩大，并已广泛应用于药物分析、生化分析等多个领域。

生物活性

Luminol钠盐是一种化学发光物质，pKa值分别为6.74和15.1。Luminol钠盐的最佳荧光波长为425 nm，常被用作法医检测血迹的诊断工具，在刑事侦查、生物工程及化学示踪等领域中发挥重要作用。

体外研究

鲁米诺浓度是影响化学发光（CL）强度的重要因素。鲁米诺化学发光（LCL）的强度不仅取决于鲁米诺自身浓度，还与氧化剂浓度、酶浓度以及pH值等其他因素有关。记录到的最大CL强度出现在0.3 mM鲁米诺浓度下。在0.01至0.3 mM范围内，随着鲁米诺浓度增加，CL强度呈线性增长。然而，进一步提高鲁米诺浓度会导致CL强度下降。

文献信息

• Preparation of high purity phenothiazine N-alkylsulfonates and their use in chemiluminescent assays for the measurement of peroxidase acitivity
  申请人：Della Ciana Leopoldo

  公开号：US20080176251A1

  公开（公告）日：2008-07-24

  A process is described for preparing, efficiently and with a high degree of purity N-alkylsulfonates of phenothiazine. The process consists in (a) the preparation of the phenothiazine anion, and (b) the reaction of said anion with cyclic alkyl sulfonates, such as 1,3-propane sultone and 1,4-butane sultone. This process is simpler, more direct, and more efficient than the procedures currently used for the synthesis of N-alkylsulfonates derivatives of phenothiazine. In addition, the products obtained with this process are far more pure than those obtained through current procedures and therefore ideal for bioanalytical applications that require high sensitivity, such as assays based on the measurement of peroxidase activity using chemiluminescence.

  描述了一种制备苯并噻嗪N-烷基磺酸盐的过程，高效且纯度较高。该过程包括(a)制备苯并噻嗪负离子，以及(b)将该负离子与环状烷基磺酸盐（如1,3-丙烷磺酸内酯和1,4-丁烷磺酸内酯）反应。这一过程比目前用于合成苯并噻嗪N-烷基磺酸盐衍生物的程序更简单、更直接、更高效。此外，用这一过程得到的产品比通过当前程序得到的产品更纯，因此非常适合需要高灵敏度的生物分析应用，如基于化学发光法测定过氧化物酶活性的分析。
• CRYSTALLINE FORMS FOR 5-AMINO-2, 3-DIHYDROPHTHALAZINE-1, 4-DIONE SODIUM SALT, PHARMACEUTICAL PREPARATIONS CONTAINING THE SAME AND METHOD FOR THE PRODUCTION OF SAID FORMS
  申请人：Breu Josef

  公开号：US20120329801A1

  公开（公告）日：2012-12-27

  The invention relates to the provision of two novel crystalline forms I and II for 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt. Surprisingly, it was discovered that form I and form II have differing immunological effects. This advantageous property is useful for immunospecific applications. In addition, both forms have advantageous physicochemical properties, which are useful in the production, further processing and/or use of a pharmaceutical preparation of form I or form II or a mixture of both.

  本发明涉及为5-氨基-2,3-二氢鞣酸1,4-二酮钠盐提供两种新的晶体形式I和II。令人惊讶的是，发现I和II形式具有不同的免疫学效果。这种有利的性质对于免疫特异性应用非常有用。此外，这两种形式具有有利的物理化学性质，对于制备、进一步加工和/或使用I或II形式或两者的混合物的制药制剂非常有用。
• NEW METHOD FOR OBTAINING 5-AMINO 2,3-DIHYDROPHTHALAZINE-1,4-DIONE ALKALI METAL SALTS AND THEIR USE IN MEDICINE
  申请人：Abidov Admir Musaevich

  公开号：US20110275642A1

  公开（公告）日：2011-11-10

  The invention is related to a method for preparing 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals of the formula II wherein 5-nitro-2,3-dihydrophthalazine-1,4-dione is solved in water solution of MOH1 where M has the below mentioned meaning, with formation of solution of 5-nitro-2,3-dihydrophthalazine-1,4-dione alkali metal salt, which is catalytically transformed into 5-amino-2,3-dihydrophthalazine-1,4-dione salt at the temperature 40-900C by means of hydrogen under the pressure 1-4 MPa in at the presence of a transition metal catalyst (Pt, Pd) on activated carbon, and separation of crystalline 5-amino-2,3-dihydrophthalazine-1,4-dione salt is performed by water solution diluting with lower alcohol or cyclic lower ether with cooling to the temperature −5° C. to −15° C., providing that there is used 5-nitro-2,3-dihydrophthalazine-1,4-dione formed in the reaction of anhydride of 3-nitrophthalic acid with hydrazine hydrate in anhydrous acetic acid at the temperature 100-110° C. with distilling the mixture of acetic acid and water off. There was also presented a pharmaceutical composition containing such obtained 5-amino-2,3-dihydrophthalazine-1,4-dione salt with alkali metals and its application in medicine. There was also presented new use of 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt for production of a drug for treatment of heart diseases, pancreas diseases and diabetes as well as application of sodium salt optionally in combination with lithium salt for treatment of the nervous system diseases. Besides, the methods of treatment of these diseases were also presented. Formula II where M represents Li, Na, K

  该发明涉及一种制备式II的碱金属5-氨基-2,3-二氢酞嗪-1,4-二酮盐的方法，其中5-硝基-2,3-二氢酞嗪-1,4-二酮溶于MOH1的水溶液中，其中M具有下面所述的含义，形成5-硝基-2,3-二氢酞嗪-1,4-二酮碱金属盐的溶液，该溶液在存在过渡金属催化剂（Pt，Pd）和活性炭的条件下，在温度40-900C下通过氢气催化转化为5-氨基-2,3-二氢酞嗪-1,4-二酮盐，在冷却至温度-5°C至-15°C的情况下，通过将水溶液稀释至低级醇或环状低级醚中，分离出结晶的5-氨基-2,3-二氢酞嗪-1,4-二酮盐，前提是在无水乙酸中，通过3-硝基苯甲酸酐与肼水合物的反应，在温度100-110°C下蒸馏掉乙酸和水的混合物中形成5-硝基-2,3-二氢酞嗪-1,4-二酮。还提供了含有所获得的碱金属5-氨基-2,3-二氢酞嗪-1,4-二酮盐的制药组合物及其在医学上的应用。还提供了5-氨基-2,3-二氢酞嗪-1,4-二酮钠盐用于治疗心脏疾病、胰腺疾病和糖尿病的药物的新用途，以及钠盐与锂盐的组合治疗神经系统疾病的应用。此外，还提供了治疗这些疾病的方法。其中M代表Li，Na，K。
• PHARMACEUTICAL GRADE PHTHALAZINEDIONES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：BACH PHARMA, INC

  公开号：US20160237039A1

  公开（公告）日：2016-08-18

  The present invention comprises methods of manufacturing a highly purified, pharmaceutical grade phthalazinedione for administration to a human or animal. The manufacturing methods identify and isolate starting materials, and prepare intermediate products, which are suitable for the commercial batch process production of highly purified and high-yielding intermediate products and final phthalazinedione products.

  本发明涉及制造高纯度、制药级邻苯二酮衍生物的方法，以供人类或动物使用。制造方法通过识别和分离起始材料，并制备中间产物，适用于商业批量生产高纯度和高产率的中间产物和最终邻苯二酮衍生物产品。
• MEDICINAL PREPARATION AND PROCESS FOR MANUFACTURING THEREOF
  申请人：——

  公开号：US20020198208A1

  公开（公告）日：2002-12-26

  The present invention can be used in medical practice specifically in chemical and pharmaceutical production of medicinal agents capable of modulating the immune system. This invention essentially relates to a new medicinal preparation 5 -amino- 2,3 -dihydrophthalazine- 1,4 -dione sodium salt having immunomodulatory, antiinflammatory, and antioxidant properties. The preparation is obtained from 3 -nitro-phthalanhydride by consecutive isolation of intermediate and end products. The intermediate products include 5 -nitro- 2,3 -dihydrophthalazine- 1,4 -dione and 5 -amino- 2,3 -dihydrophthala 2 ine- 1,4 -dione. The reaction between 5 -amino- 2,3 -dihydrophthalazine- 1,4 -dione and sodium hydroxide yields the target product, 5 -animo- 2,3 -dihydrophthalazine- 1,4 -dione sodium salt. The method allows to produce the medicinal preparation with high pharmaceutical activity. It is provided an example of application of this preparation.

  本发明可用于医学实践，特别是用于调节免疫系统的药物的化学和制药生产。本发明主要涉及一种新的药物制剂——5-氨基-2,3-二氢酞嗪-1,4-二酮钠盐，具有免疫调节、抗炎和抗氧化性能。该制备物是通过连续分离中间产物和终产物从3-硝基酞酰亚胺中获得的。中间产物包括5-硝基-2,3-二氢酞嗪-1,4-二酮和5-氨基-2,3-二氢酞嗪-1,4-二酮。5-氨基-2,3-二氢酞嗪-1,4-二酮和氢氧化钠之间的反应产生目标产物——5-氨基-2,3-二氢酞嗪-1,4-二酮钠盐。该方法允许以高药物活性生产药物制剂。提供了该制备物的应用示例。