利血那明 | 24815-24-5

• 物质功能分类: 生物化工 - 中草药成分
• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 育亨宾生物碱
• 中文名称: 利血那明
• 中文别名: 利血胺
• 英文名称: rescinnamine
• 英文别名: Cinnaloid；resciimamin；reserpinine；11,17-dimethoxy-18-[3-(3,4,5-trimethoxy-phenyl)-acryloyloxy]-yohimbane-16-carboxylic acid methyl ester；ent-11,17β-dimethoxy-18α-(3,4,5-trimethoxy-trans-cinnamoyloxy)-15β-yohimban-16α-carboxylic acid methyl ester；methyl (1R,15S,17R,18R,19S,20S)-6,18-dimethoxy-17-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]oxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate
• CAS: 24815-24-5
• 化学式: C₃₅H₄₂N₂O₉
• 分子量: 634.726
• InChiKey: SZLZWPPUNLXJEA-QEGASFHISA-N

物化性质

• 熔点：
  238-239°C
• 比旋光度：
  D24 -97° (c = 1 in chloroform)
• 沸点：
  669.26°C (rough estimate)
• 密度：
  1.2161 (rough estimate)
• 溶解度：
  氯仿（微溶）、甲醇（微溶、加热）
• 物理描述：
  Rescinnamine is an odorless white to cream colored crystalline powder. (NTP, 1992)
• 颜色/状态：
  Fine needles from benzene
• 气味：
  ODORLESS
• 稳定性/保质期：

  DARKENS SLOWLY ON EXPOSURE TO LIGHT, MORE RAPIDLY WHEN IN SOLN.

• 旋光度：
  Specific optical rotation: -97 deg @ 24 °C/D (c= 1 in chloroform); UV max absorption (methanol): 228, 302 nm (log e= 4.79, 4.48)

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  46
• 可旋转键数：
  11
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.49
• 拓扑面积：
  118
• 氢给体数：
  1
• 氢受体数：
  10

ADMET

毒理性

• 解毒与急救

治疗：3. 上腹部疼痛与...消化性溃疡可能需要局部抗酸治疗... 4. ...运动功能障碍...通常可以通过用于治疗...帕金森病的药物来控制，但更安全的方法是停止使用利血平治疗... /利血平/

TREATMENT: 3. EPIGASTRIC PAIN &...PEPTIC ULCER MAY REQUIRE LOCAL ANTACID THERAPY... 4. ...MOTOR DYSFUNCTION...OFTEN CONTROLLED BY DRUGS USEFUL...IN PARKINSONISM, BUT SAFER COURSE IS TO DISCONTINUE RESERPINE THERAPY... /RESERPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

治疗：5. 对于急性中毒的患者...如果患者没有昏迷，催吐...或者洗胃...即使摄入数小时后...在胃中留下盐水泻药。6. ...昏迷伴低血压...对保守支持性治疗有反应。中枢兴奋药...可能比有益的更危险... /利血平/

TREATMENT: 5. IN ACUTELY POISONED PT...NOT IN COMA, EMESIS...OR GASTRIC LAVAGE...EVEN SEVERAL HR AFTER INGESTION... LEAVE SALINE CATHARTIC IN STOMACH. 6. ...COMA WITH HYPOTENSION...RESPONDS TO CONSERVATIVE SUPPORTIVE THERAPY. ANALEPTIC DRUGS...PROBABLY MORE DANGEROUS THAN BENEFICIAL... /RESERPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

治疗：7. 使用毯子和外部热量来维持体温... 8. 除非血压变得非常低，否则避免使用血管收缩药物...可能导致心血管反应过度... 9. 由于心脏状况不确定...避免快速静脉输液... /利血平/

TREATMENT: 7. USE BLANKETS &...EXTERNAL...HEAT TO MAINTAIN BODY TEMP... 8. UNLESS BLOOD PRESSURE BECOMES VERY LOW, AVOID VASOPRESSOR DRUGS... MAY LEAD TO EXAGGERATED CARDIOVASCULAR RESPONSE... 9. BECAUSE OF UNCERTAIN CARDIAC STATUS...AVOID RAPID IV INFUSIONS... /RESERPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

治疗：10.尽管在临床中毒病例中并未描述，但使用哇巴因或乙酰毛花苷快速进行数字化处理可能有助于...维持足够的循环，尽管这可能会增加心脏心律不齐的高风险。/利血平/

TREATMENT: 10. ALTHOUGH NOT DESCRIBED IN CLINICAL POISONINGS, RAPID DIGITALIZATION WITH OUABAIN OR ACETYLSTROPHANTHIDIN MAY AID...ADEQUATE CIRCULATION, ALTHOUGH THERE MAY BE HIGH RISK OF CARDIAC ARRHYTHMIAS. /RESERPINE/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

见利血平生物碱。建议使用拟交感神经药物，如甲基苯丙胺，作为过量治疗的药物。/利血平生物碱/

SEE RAUWOLFIA ALKALOIDS. A SYMPATHOMIMETIC...SUCH AS METHAMPHETAMINE IS SUGGESTED TREATMENT FOR OVERDOSAGE. /RAUWOLFIA ALKALOIDS/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

RAUWOLFIA ALKALOIDS ARE ABSORBED READILY FROM GI TRACT & FROM PARENTERAL SITES OF INJECTION. 瑞沃夫碱（RAuwolfia AlkALOids）容易从胃肠道和注射部位被吸收。

RAUWOLFIA ALKALOIDS ARE ABSORBED READILY FROM GI TRACT & FROM PARENTERAL SITES OF INJECTION.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

见利血平生物碱。可穿过胎盘屏障，可能影响新生儿。/利血平生物碱/

SEE RAUWOLFIA ALKALOIDS. ...PASS PLACENTAL BARRIER & MAY AFFECT NEWBORN. /RAUWOLFIA ALKALOIDS/

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• 危险等级：
  6.1(b)
• 危险品标志：
  Xn
• 安全说明：
  S22,S36,S45
• 危险类别码：
  R20/21/22,R25
• 危险品运输编号：
  UN 1544
• 包装等级：
  III
• 危险类别：
  6.1(b)

反应信息

• 作为反应物：
  描述：

  利血那明 在 palladium on activated charcoal 氢气 作用下， 以 乙醇 为溶剂， 反应 24.0h， 生成 ent-11,17β-dimethoxy-18α-[3-(3,4,5-trimethoxy-phenyl)-propionyloxy]-15β-yohimban-16α-carboxylic acid methyl ester
  参考文献：
  名称：

  Bhat; Winter, Mark A.; Pearce, Molecular Pharmacology, 1995, vol. 48, # 4, p. 682 - 689

  摘要：

  DOI：
• 作为产物：
  描述：

  (E)-3-(3,4,5-trimethoxyphenyl)acryloyl chloride 、 (3beta,16beta,17alpha,18beta,20alpha)-18-羟基-11,17-二甲氧基育亨宾-16-羧酸甲酯 生成 利血那明
  参考文献：
  名称：

  US2854454

  摘要：

  公开号：

文献信息

• BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1422228A1

  公开（公告）日：2004-05-26

  The present invention provides a novel benzazepine derivative represented by formula : wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.

  本发明提供了一种新型的苯并氮杂环衍生物，其由以下公式表示： 其中，R1是一个5-或6-成员的芳香环，R2是低级烷基团等，Y是可选地取代的亚氨基，环A和环B是独立地选自一个可选地取代的芳香环，W是公式-W1-X2-W2-（W1和W2是独立地为S(O)m1（m1是0、1或2）等，X2是一个可选地取代的亚烷基团等），其制备方法及其用途。
• GLUTATHIONE-CHOLESTEROL DERIVATIVES AS BRAIN TARGETING AGENTS
  申请人：South Dakota Board of Regents

  公开号：US20200048305A1

  公开（公告）日：2020-02-13

  The present invention describes compositions containing cholesterol-linker-glutathione conjugates for targeting the brain by overcoming barrier entry to the CNS through the blood brain barrier (BBB), including micelle and liposome forms of such compositions. In addition, methods for treating subjects by administering such compositions are also disclosed.

  本发明描述了含有胆固醇-连接剂-谷胱甘肽共轭物的组合物，通过克服血脑屏障（BBB）进入中枢神经系统的屏障入口，包括这些组合物的胶束和脂质体形式。此外，还公开了通过给予这些组合物治疗受试者的方法。
• Sulfonyl-containing 2,3-diarylindole compounds, methods for making same, and methods of use thereof
  申请人：——

  公开号：US20040058977A1

  公开（公告）日：2004-03-25

  The present invention relates to sulfonyl-containing 2,3-diarylindole, especially to new compounds of general Formula, to a preparation method for their preparation, to pharmaceutical compositions containing said compound, and to the medical use thereof in the treatment of diseases relating to the inhibition of cyclooxygenase-2 (COX-2).

  本发明涉及含砜基的2,3-二芳基吲哚，特别涉及一般式的新化合物，其制备方法，含有该化合物的药物组合物，以及在治疗与环氧合酶-2（COX-2）抑制有关的疾病中的医疗用途。
• Heterocyclic compounds
  申请人：Yamamoto Hiroshi

  公开号：US20070072908A1

  公开（公告）日：2007-03-29

  The present invention provides a compound represented by the following formula [1′] or a salt thereof: wherein ring A, R 2 , R 3 , R 4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11βHSD1 inhibitor, containing the compound or a salt thereof.

  本发明提供了由以下式[1']表示的化合物或其盐： 其中环A，R2，R3，R4和X如描述中所定义，并且包含该化合物或其盐的用于治疗或预防涉及糖皮质激素的病理或11βHSD1抑制剂的药剂。
• [EN] PYRAZOLO [4, 3-D] PYRIMIDINES USEFUL AS KINASE INHIBITORS<br/>[FR] PYRAZOLO[4,3-D]PYRIMIDINES UTILES EN TANT QU'INHIBITEURS DE KINASES
  申请人：ORIGENIS GMBH

  公开号：WO2012143144A1

  公开（公告）日：2012-10-26

  The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

  本发明涉及一种能够抑制一个或多个激酶，特别是SYK（脾酪氨酸激酶）、LRRK2（富含亮氨酸重复的激酶2）和/或MYLK（肌球蛋白轻链激酶）或其突变体的化合物的新颖化合物（I）的公式。这些化合物在治疗各种疾病中发挥作用。这些疾病包括自身免疫疾病、炎症性疾病、骨疾病、代谢性疾病、神经和神经退行性疾病、癌症、心血管疾病、过敏、哮喘、阿尔茨海默病、帕金森病、皮肤疾病、眼部疾病、传染病和与激素相关的疾病。