肾上腺素 | 51-43-4

• 物质功能分类: 原料药 - 循环系统用药 - 抗休克血管活性药
• 分子结构分类: 有机化合物 - 苯类化合物 - 酚类
• 中文名称: 肾上腺素
• 中文别名: (R)-肾上腺素；L-3,4-二羟基-alpha-((甲氨基)甲基)苄醇；L-肾上腺素盐酸盐单水合物；L-肾上腺素；L(-)-肾上腺素；肾上腺激素；副肾碱；(-)-肾上腺素；副肾素；肾副素；肾副碱；负肾素
• 英文名称: L-epinephrine
• 英文别名: Epinephrine；3,4-dihydroxy-α-[(methylamino)methyl]benzyl alcohol；(R)-4-[1-hydroxy-2-(methylamino)ethyl]-1,2-benzenediol；adrenaline；L-adrenaline；adrenalin；2-hydroxy-4-[(1R)-1-hydroxy-2-(methylazaniumyl)ethyl]phenolate
• CAS: 51-43-4
• 化学式: C₉H₁₃NO₃
• mdl: MFCD00002204
• 分子量: 183.207
• InChiKey: UCTWMZQNUQWSLP-VIFPVBQESA-N

物化性质

• 熔点：
  215 °C (dec.)(lit.)
• 比旋光度：
  -51.5 º (c=4, 1M HCl, dry sub)
• 沸点：
  316.88°C (rough estimate)
• 密度：
  1.1967 (rough estimate)
• 溶解度：
  几乎不溶于水、乙醇（96%）和二氯甲烷。溶于盐酸。
• 物理描述：
  Solid
• 颜色/状态：
  Brown (in air)
• 气味：
  Odorless
• 蒸汽压力：
  7.37X10-8 mm Hg at 25 °C (est)
• 亨利常数：
  Henry's Law constant = 7.06X10-19 atm-cu m/mol at 25 °C (est)
• 稳定性/保质期：

  In some commercially available injections, the air has been replaced with nitrogen to avoid oxidation. Withdrawal of doses from multiple-dose vials introduces air into the vials, subjecting the remaining epinephrine to oxidation. Oxidation of the drug imparts first a pink, then a brown color; epinephrine preparations must not be used if they have a pinkish or darker than slightly yellow color or contain a precipitate.

• 旋光度：
  Specific optical rotation = -50 deg to -53.3 deg at 25 °C/D (in 0.6N HCl)
• 分解：
  When heated to decomposition it emits toxic fumes of /nitrogen oxides/.
• Caco2细胞的药物渗透性：
  -6.02
• 解离常数：
  8.59 (at 25 °C)
• 碰撞截面：
  138.3 Ų [M+H-H2O]+ [CCS Type: DT, Method: single field calibrated with Agilent tune mix (Agilent)]

计算性质

• 辛醇/水分配系数(LogP)：
  -1.4
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  72.7
• 氢给体数：
  4
• 氢受体数：
  4

ADMET

代谢

肾上腺素主要通过酶促转化成甲基肾上腺素或去甲肾上腺素而迅速失活，之后这两种物质会被结合并随尿液以硫酸盐和葡萄糖醛酸苷的形式排出体外。这两个过程最终都会形成3-甲氧基-4-羟基扁桃酸（香草扁桃酸，VMA），这种物质在尿液中是可以检测到的。肾上腺素在体内迅速失活主要是通过COMT（儿茶酚-O-甲基转移酶）和MAO（单胺氧化酶）这两种酶。肝脏富含上述酶类，是肾上腺素降解过程的主要但非必需的组织。

Epinephrine is rapidly inactivated mainly by enzymic transformation to metanephrine or normetanephrine, either of which is then conjugated and excreted in the urine in the form of both sulfates and glucuronides. Either sequence results in the formation of 3-methoxy-4- hydroxy-mandelic acid(vanillylmandelic acid, VMA) which is shown to be detectable in the urine. Epinephrine is rapidly inactivated in the body mostly by the enzymes COMT (catechol-O-methyltransferase) and MAO (monoamine oxidase). The liver is abundant in the above enzymes, and is a primary, although not essential, tissue in the degradation process.

来源:DrugBank

代谢

肾上腺素的药理作用主要通过在交感神经末梢的摄取和代谢来终止。循环中的药物在肝脏和其他组织中通过涉及酶儿茶酚-O-甲基转移酶（COMT）和单胺氧化酶（MAO）的多种反应来代谢。主要代谢物是去甲肾上腺素和对羟基苯乙酸（香草扁桃酸，VMA），这两种物质都是无活性的。大约40%的肾上腺素注射剂量以去甲肾上腺素形式从尿液中排出，40%以VMA形式排出，7%以3-甲氧基-4-羟基苯乙二醇形式排出，2%以3,4-二羟基苯乙酸形式排出，其余以乙酰化衍生物形式排出。这些代谢物主要以硫酸盐结合物形式排出，较少部分以葡萄糖醛酸结合物形式排出。只有少量药物以原形排出。

The pharmacologic actions of epinephrine are terminated mainly by uptake and metabolism in sympathetic nerve endings. Circulating drug is metabolized in the liver and other tissues by a combination of reactions involving the enzymes catechol-O-methyltransferase (COMT) and monoamine oxidase (MAO). The major metabolites are metanephrine and 3-methoxy-4-hydroxymandelic acid (vanillylmandelic acid, VMA) both of which are inactive. About 40% of a parenteral dose of epinephrine is excreted in urine as metanephrine, 40% as VMA, 7% as 3-methoxy-4-hydroxyphenoglycol, 2% as 3,4-dihydroxymandelic acid, and the remainder as acetylated derivatives. These metabolites are excreted mostly as the sulfate conjugates and, to a lesser extent, the glucuronide conjugates. Only small amounts of the drug are excreted unchanged.

来源:Hazardous Substances Data Bank (HSDB)

代谢

循环中的肾上腺素在肝脏中被代谢，并进入肾上腺素能神经元，在单胺氧化酶（MAO）和儿茶酚-O-甲基转移酶的作用下被代谢为去甲肾上腺素、硫酸盐结合物和MAndelic酸的水解衍生物。

Circulating epinephrine is metabolized in the liver and is taken up into adrenergic neurons and metabolized by MAO and catechol-O-methyltransferase to metadrenaline, sulfate conjugates, and hydroxy derivatives of mandelic acid.

来源:Hazardous Substances Data Bank (HSDB)

代谢

肾上腺素有人类已知的代谢物，包括硫酸肾上腺素。

Epinephrine has known human metabolites that include Epinephrine sulfate.

来源:NORMAN Suspect List Exchange

毒理性

• 药物性肝损伤

化合物：肾上腺素

Compound:epinephrine

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

DILI 注解：无 DILI（药物性肝损伤）担忧

DILI Annotation:No-DILI-Concern

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

标签部分：没有匹配项

Label Section:No match

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 药物性肝损伤

参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 用于研究药物诱导肝损伤的FDA批准药物标签，药物发现今天，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按发展药物诱导人类肝损伤风险排名的最大参考药物清单。药物发现今天2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015

来源:Drug Induced Liver Injury Rank (DILIrank) Dataset

毒理性

• 在妊娠和哺乳期间的影响

◉ 母乳喂养期间使用概要：目前没有关于在哺乳期间使用肾上腺素的信息。由于其口服生物利用度低和半衰期短，乳中的肾上腺素不太可能影响婴儿。高剂量的静脉注射肾上腺素可能会减少乳汁产量或乳汁排放。低剂量的肌内注射（如Epi-Pen）、硬脊膜外、局部、吸入或眼用肾上腺素不太可能干扰哺乳。为了在使用眼药水后显著减少药物的效果，可以在眼角处按压泪囊1分钟或更长时间，然后用吸收性纸巾去除多余的溶液。肾上腺素是治疗过敏性休克的首先药物，应该在哺乳和非哺乳患者中以相同的方式使用。 ◉ 对哺乳婴儿的影响：截至修订日期，没有找到相关的已发布信息。 ◉ 对泌乳和母乳的影响：截至修订日期，没有在哺乳母亲中找到相关的已发布信息。在非哺乳受试者和高催乳素血症女性中，静脉输注肾上腺素会降低血清催乳素浓度。动物数据显示，动脉内注射肾上腺素可以降低血清催乳素并抑制乳汁排放。然而，作为硬脊膜外镇痛一部分的低剂量肾上腺素输注并不会影响哺乳母亲的哺乳。在已建立泌乳的母亲中，催乳素水平可能不会影响她的哺乳能力。 一项埃及研究比较了75名接受2%利多卡因（n = 75）和70名接受2%利多卡因加1:200,000肾上腺素（n = 70）作为剖宫产后伤口浸润的效果。接受肾上腺素与利多卡因联合使用的患者在手术后89分钟开始哺乳，而仅接受利多卡因的患者在132分钟开始哺乳。这个差异在统计学上是显著的。

◉ Summary of Use during Lactation:No information is available on the use of epinephrine during breastfeeding. Because of its poor oral bioavailability and short half-life, any epinephrine in milk is unlikely to affect the infant. High intravenous doses of epinephrine might reduce milk production or milk letdown. Low-dose intramuscular (such as Epi-Pen), epidural, topical, inhaled or ophthalmic epinephrine are unlikely to interfere with breastfeeding. To substantially diminish the effect of the drug after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue. Epinephrine is the first line-medication of choice for treatment of anaphylaxis; it should be used in the same manner in breastfeeding and non-breastfeeding patients. ◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk:Relevant published information in nursing mothers was not found as of the revision date. Intravenous epinephrine infusion in nonnursing subjects and in women with hyperprolactinemia decreases serum prolactin concentrations. Animal data indicate that intraarterial epinephrine can decrease serum oxytocin and inhibit milk ejection. However, low-dose infusion of epinephrine as part of epidural analgesia does not impair breastfeeding in nursing mothers. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. An Egyptian study compared lidocaine 2% (n = 75) to lidocaine 2% plus epinephrine 1:200,000 (n = 70) as a wound infiltration following cesarean section. Patients who received epinephrine in combination with lidocaine began breastfeeding at 89 minutes following surgery compared to 132 minutes for those receiving lidocaine alone. The difference was statistically significant.

来源:Drugs and Lactation Database (LactMed)

吸收、分配和排泄

• 吸收

静脉注射后，肾上腺素会迅速从血液中消失。皮下或肌肉注射的肾上腺素具有快速起效和短时作用的特点。在哮喘发作期间，皮下给药可能在5到10分钟内产生支气管扩张，最大效果可能在20分钟内出现。药物会迅速固定在组织中。

Following I.V. (intravenous) injection, epinephrine disappears rapidly from the blood stream. Subcutaneously or I.M. (intramuscular) administered epinephrine has a rapid onset and short duration of action. Subcutaneous (SC) administration during asthmatic attacks may produce bronchodilation within 5 to 10 minutes, and maximal effects may occur within 20 minutes. The drug becomes fixed in the tissues rapidly,.

来源:DrugBank

吸收、分配和排泄

• 消除途径

肾上腺素剂量的多数通过尿液排出。大约40%的肾上腺素通过尿液以去甲肾上腺素形式排出，40%以VMA形式排出，7%以3-甲氧基-4-羟基苯乙醇形式排出，2%以3,4-二羟基苯乙酸形式排出，其余以乙酰化衍生物形式排出。这些代谢物主要以硫酸盐结合物形式排出，其次是以葡萄糖醛酸结合物形式排出。只有少量药物完全不变地排出。

The majority of the dose of epinephrine is seen excreted in the urine,. About 40% of a parenteral dose of epinephrine is excreted in urine as metanephrine, 40% as VMA, 7% as 3-methoxy-4-hydroxyphenoglycol, 2% as 3,4-dihydroxymandelic acid, and the rest as acetylated derivatives. These metabolites are excreted mainly as the sulfate conjugates and, to a lesser extent, the glucuronide conjugates. Only small amounts of the drug are excreted completely unchanged.

来源:DrugBank

吸收、分配和排泄

• 清除

静脉注射会产生立即和加强的反应。静脉注射后，肾上腺素会迅速从血液中消失。

Intravenous injection produces an immediate and intensified response. Following intravenous injection, epinephrine disappears rapidly from the blood stream.

来源:DrugBank

吸收、分配和排泄

在兔眼局部应用放射性标记肾上腺素后，除眼以外组织和液体中药物浓度最高的是垂体腺，其次是肠道、脂肪、肾上腺、肾脏、心脏、肺、脾、卵巢、胰腺、肝脏、子宫、肌肉、大脑和血清。在人类中，系统吸收的肾上腺素可以穿过胎盘，但不能穿过血脑屏障。系统吸收的肾上腺素会分布到乳汁中。

Following topical application of radiolabeled epinephrine to the eye in rabbits, highest concentrations of the drug in tissues and fluids other than the eye occurred in the pituitary gland, with lower concentrations in the intestine, fat, adrenal gland, kidney, heart, lung, spleen, ovary, pancreas, liver, uterus, muscle, brain, and serum. In humans, systemically absorbed epinephrine crosses the placenta but not the blood-brain barrier. Systemically absorbed epinephrine distributes into milk.

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

肾上腺素口服给药后无效，因为它在胃肠道粘膜和肝脏中迅速结合和氧化。由于局部血管收缩，从皮下组织的吸收发生缓慢...肌内注射后的吸收比皮下注射后的吸收更快...肾上腺素在体内迅速失活。

Epinephrine is not effective after oral admin because it is rapidly conjugated and oxidized in GI mucosa and liver. Absorption from sc tissues occurs slowly because of local vasoconstriction ... Absorption is more rapid after im than after sc injection ... Epinephrine is rapidly inactivated in the body.

来源:Hazardous Substances Data Bank (HSDB)

安全信息

• TSCA：
  Yes
• 危险等级：
  6.1
• 危险品标志：
  T
• 安全说明：
  S23,S26,S36/37/39,S45,S61
• 危险类别码：
  R23/24/25,R36/37/38,R52/53,R33
• WGK Germany：
  3
• 海关编码：
  2922509090
• 危险品运输编号：
  UN 2811
• 危险类别：
  6.1
• RTECS号：
  DO2625000
• 包装等级：
  II
• 储存条件：
  充氮密封、阴凉避光保存。

SDS

Name:	Adrenaline Material Safety Data Sheet
Synonym:	Epinephrine; Adrenal; 1-Adrenaline; Adrenaso
CAS:	51-43-4

Section 1 - Chemical Product MSDS Name:Adrenaline Material Safety Data Sheet
Synonym:Epinephrine; Adrenal; 1-Adrenaline; Adrenaso

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Section 2 - COMPOSITION, INFORMATION ON INGREDIENTS

CAS#	Chemical Name	content	EINECS#
51-43-4	1,2-benzenediol, 4-[1-hydroxy-2-(methy	100%	200-098-7

Hazard Symbols: T
Risk Phrases: 23/24/25 33

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Section 3 - HAZARDS IDENTIFICATION
EMERGENCY OVERVIEW
Toxic by inhalation, in contact with skin and if swallowed. Danger of cumulative effects.Toxic.
Potential Health Effects
Eye:
May cause eye irritation. No information regarding eye irritation and other potential effects was found.
Skin:
May cause skin irritation. No information regarding skin irritation and other potential effects was found.
Ingestion:
Causes gastrointestinal irritation with nausea, vomiting and diarrhea.
Inhalation:
May cause respiratory tract irritation. Overexposure may cause dizziness, tremors, restlessness, rapid heart beat, increased blood pressure, hallucinations, acidosis, kidney failure.
Chronic:
Not available.

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Section 4 - FIRST AID MEASURES
Eyes: Flush eyes with plenty of water for at least 15 minutes, occasionally lifting the upper and lower eyelids. Get medical aid.
Skin:
Get medical aid. Flush skin with plenty of water for at least 15 minutes while removing contaminated clothing and shoes.
Ingestion:
If victim is conscious and alert, give 2-4 cupfuls of milk or water.
Never give anything by mouth to an unconscious person. Get medical aid immediately.
Inhalation:
Remove from exposure and move to fresh air immediately. If not breathing, give artificial respiration. If breathing is difficult, give oxygen. Get medical aid.
Notes to Physician:

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Section 5 - FIRE FIGHTING MEASURES
General Information:
As in any fire, wear a self-contained breathing apparatus in pressure-demand, MSHA/NIOSH (approved or equivalent), and full protective gear.
Extinguishing Media:
For small fires, use water spray, dry chemical, carbon dioxide or chemical foam.

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Section 6 - ACCIDENTAL RELEASE MEASURES
General Information: Use proper personal protective equipment as indicated in Section 8.
Spills/Leaks:
Sweep up or absorb material, then place into a suitable clean, dry, closed container for disposal. Avoid generating dusty conditions.

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Section 7 - HANDLING and STORAGE
Handling:
Wash thoroughly after handling. Wash hands before eating. Remove contaminated clothing and wash before reuse. Use with adequate ventilation. Do not get on skin or in eyes. Do not ingest or inhale.
Storage:
Keep away from heat and flame. Store in a cool, dry, well-ventilated area away from incompatible substances. Keep containers tightly closed.

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Section 8 - EXPOSURE CONTROLS, PERSONAL PROTECTION
Engineering Controls:
Use adequate ventilation to keep airborne concentrations low.
Exposure Limits CAS# 51-43-4: Personal Protective Equipment Eyes: Wear appropriate protective eyeglasses or chemical safety goggles as described by OSHA's eye and face protection regulations in 29 CFR 1910.133 or European Standard EN166.
Skin:
Wear appropriate protective gloves to prevent skin exposure.
Clothing:
Wear appropriate protective clothing to prevent skin exposure.
Respirators:
Follow the OSHA respirator regulations found in 29 CFR 1910.134 or European Standard EN 149. Use a NIOSH/MSHA or European Standard EN 149 approved respirator if exposure limits are exceeded or if irritation or other symptoms are experienced.

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Section 9 - PHYSICAL AND CHEMICAL PROPERTIES

Physical State: Solid
Color: white
Odor: odorless
pH: Not available.
Vapor Pressure: Not available.
Viscosity: Not available.
Boiling Point: Not available.
Freezing/Melting Point: Not available.
Autoignition Temperature: Not applicable.
Flash Point: Not applicable.
Explosion Limits, lower: Not available.
Explosion Limits, upper: Not available.
Decomposition Temperature: Not available.
Solubility in water: Not available.
Specific Gravity/Density: Not available.
Molecular Formula: C9H14ClNO3
Molecular Weight: 219.5559

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Section 10 - STABILITY AND REACTIVITY
Chemical Stability:
Stable under normal temperatures and pressures.
Conditions to Avoid:
Incompatible materials.
Incompatibilities with Other Materials:
Strong oxidizers.
Hazardous Decomposition Products:
Hydrogen chloride, nitrogen oxides, carbon monoxide, carbon dioxide.
Hazardous Polymerization: Has not been reported.

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Section 11 - TOXICOLOGICAL INFORMATION
RTECS#:
CAS# 51-43-4: DO2625000 LD50/LC50:
CAS# 51-43-4: Skin, rat: LD50 = 62 mg/kg.
Carcinogenicity:
1,2-benzenediol, 4-[1-hydroxy-2-(methylamino)ethyl] - Not listed by ACGIH, IARC, or NTP.
Other:
See actual entry in RTECS for complete information.

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Section 12 - ECOLOGICAL INFORMATION

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Section 13 - DISPOSAL CONSIDERATIONS
Products which are considered hazardous for supply are classified as Special Waste and the disposal of such chemicals is covered by regulations which may vary according to location. Contact a specialist disposal company or the local waste regulator for advice. Empty containers must be decontaminated before returning for recycling.

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Section 14 - TRANSPORT INFORMATION

IATA
Shipping Name: ALKALOIDS, SOLID, NOS((-)-Adrenaline)
Hazard Class: 6.1
UN Number: 1544
Packing Group: II
IMO
Shipping Name: ALKALOIDS, SOLID, NOS((-)-Adrenaline)
Hazard Class: 6.1
UN Number: 1544
Packing Group: II
RID/ADR
Shipping Name: ALKALOIDS, SOLID, NOS((-)-Adrenaline)
Hazard Class: 6.1
UN Number: 1544
Packing group: II
USA RQ: CAS# 51-43-4: 1000 lb final RQ; 454 kg final RQ

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Section 15 - REGULATORY INFORMATION

European/International Regulations
European Labeling in Accordance with EC Directives
Hazard Symbols: T
Risk Phrases:
R 23/24/25 Toxic by inhalation, in contact with skin
and if swallowed.
R 33 Danger of cumulative effects.
Safety Phrases:
S 23 Do not inhale gas/fumes/vapour/spray.
S 24/25 Avoid contact with skin and eyes.
WGK (Water Danger/Protection)
CAS# 51-43-4: 3
Canada
CAS# 51-43-4 is listed on Canada's DSL List.
CAS# 51-43-4 is not listed on Canada's Ingredient Disclosure List.
US FEDERAL
TSCA
CAS# 51-43-4 is listed on the TSCA inventory.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

根据提供的信息，我将总结肾上腺素的主要内容：

1. 药理作用：

• 心血管系统：提高心率、收缩力和血压；扩张支气管。
• 兴奋α和β受体。

2. 适应症：

• 过敏性休克
• 支气管哮喘急性发作
• 心脏骤停复苏

3. 禁忌证及慎用人群：

• 高血压、冠心病等心血管疾病患者禁用
• 糖尿病、甲状腺功能亢进等代谢性疾病患者慎用
• 急性闭角型青光眼患者禁用

4. 不良反应：

• 心悸、烦躁、震颤等交感神经兴奋症状
• 血压骤升，诱发脑出血风险
• 心律失常，严重者可致死
• 局部刺激作用：水肿、充血、炎症

5. 生产方法： 3,4-二羟基-α-甲氨基苯乙酮（肾上原酮）加氢还原生成消旋肾上腺素；经拆分、中和后得到左旋肾上腺素。

6. 化学性质与用途：

• 白色结晶性粉末，易溶于酸碱溶液
• 用于过敏性休克、支气管哮喘及心脏骤停的急救

7. 安全信息：

• 剧毒品
• 可燃物，遇火分解出有毒氮氧化物烟雾
• 应低温通风干燥保存，远离食品原料

反应信息

• 作为反应物：
  描述：

  肾上腺素 在 双氧水 、 sodium sulfate 作用下， 生成 肾上腺素红
  参考文献：
  名称：

  使用基于多两性电解质的新型钴配合物活化H 2 O 2并产生超氧化物

  摘要：

  通过对Co（II）的吸收，固态NMR和能量色散X射线分析的平衡研究，表征了一种基于Co（II）和具有聚两性电解质性质的水凝胶的新型催化剂。源自甲基丙烯酸和2-甲基咪唑的基质易于通过一站式策略合成，并将配位性能与耐化学性相结合。通过电子自旋共振研究了该材料对H 2 O 2活化的催化活性，证实了超氧自由基的释放。相互作用的可能机制涉及同时产生双氧，质子和水。在H 2 O 2活化中评估催化性能用于氧化两种与环境有关的代表性有机化合物。通过用60 mM的H 2 O 2氧化并吸附在催化剂上，在2小时内从蒸馏水中去除了约70％的甲基橙（一种偶氮染料）。在0.1 M Na 2 SO 4的存在下，染料的吸附量最小。该过程的动力学遵循伪一级经验模型，催化剂被回收再利用。选择肾上腺素作为易受超氧化物攻击的药物模型。遵循拟一级动力学模型，在不到6分钟的时间内即可达到约80％的肾上腺色素转化率。

  DOI：

  10.1016/j.apcata.2013.08.002
• 作为产物：
  描述：

  酒石酸肾上腺素 在 ammonium hydroxide 作用下， 以 水 为溶剂， 反应 3.0h， 以93%的产率得到肾上腺素
  参考文献：
  名称：

  [EN] PROCESS FOR THE PREPARATION OF OPTICALLY ENRICHED ADRENALINE
  [FR] PROCÉDÉ DE PRÉPARATION D'ADRÉNALINE ENRICHIE OPTIQUEMENT

  摘要：

  提供了一种生产(-)-肾上腺素和(-)-肾上腺素-L-酒石酸盐的过程。该过程提供了一种新的、高效且商业可行的对消旋肾上腺素进行光学分辨的方法。在一个方面，提供了一种合成(-)-肾上腺素的一锅法过程。该过程提供了一种简单且成本较低的方法，可用于制备符合API质量标准的商业规模批次的(-)-肾上腺素和(-)-肾上腺素-L-酒石酸盐。该过程避免了使用昂贵且不可预测的手性催化剂。

  公开号：

  WO2016038422A1
• 作为试剂：
  描述：

  花生四烯酸 在 Tris HCl buffer 、 谷胱甘肽 、 prostaglandin synthetase 、 肾上腺素 作用下， 反应 0.08h， 生成 前列腺素 D2 、 地诺前列酮 、 地诺前列素
  参考文献：
  名称：

  Das, Mallika; Ghosh, Dolly, Journal of the Indian Chemical Society, 1997, vol. 74, # 4, p. 319 - 322

  摘要：

  DOI：

文献信息

• [EN] TARGETED DELIVERY AND PRODRUG DESIGNS FOR PLATINUM-ACRIDINE ANTI-CANCER COMPOUNDS AND METHODS THEREOF<br/>[FR] ADMINISTRATION CIBLÉE ET CONCEPTIONS DE PROMÉDICAMENTS POUR COMPOSÉS ANTICANCÉREUX À BASE DE PLATINE ET D'ACRIDINE ET MÉTHODES ASSOCIÉES
  申请人：WAKE FOREST SCHOOL OF MEDICINE

  公开号：WO2013033430A1

  公开（公告）日：2013-03-07

  Acridine containing cispiaiin compounds have been disclosed that show greater efficacy against cancer than other cisplatin compounds. Methods of delivery of those more effective eisp!aiin compounds to the nucleus in cancer ceils is disclosed using one or more amino acids, one or more sugars, one or more polymeric ethers, C i^aikylene-phenyl-NH-C(0)-R.15, folic acid, av03 iniegriii RGD binding peptide, tamoxifen, endoxifen, epidermal growth factor receptor, antibody conjugates, kinase inhibitors, diazoles, triazol.es, oxazoies, erlotinib, and/or mixtures thereof; wherein R]§ is a peptide.

  含有环丙啶结构的吖啶类化合物已被披露，显示出比其他顺铂类化合物更有效地对抗癌症。使用一种或多种氨基酸、一种或多种糖、一种或多种聚合醚、C i^aikylene-phenyl-NH-C(0)-R.15、叶酸、av03整合RGD结合肽、他莫昔芬、恩多西芬、表皮生长因子受体、抗体结合物、激酶抑制剂、二唑类化合物、三唑类化合物、噁唑类化合物、厄洛替尼和/或它们的混合物将这些更有效的吖啶类化合物传递到癌细胞核中的方法被披露；其中R]§是一个肽。
• [EN] ACC INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE L'ACC ET UTILISATIONS ASSOCIÉES
  申请人：GILEAD APOLLO LLC

  公开号：WO2017075056A1

  公开（公告）日：2017-05-04

  The present invention provides compounds I and II useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

  本发明提供了化合物I和II，这些化合物可用作乙酰辅酶A羧化酶（ACC）的抑制剂，以及它们的组合物和使用方法。
• [EN] SULFINYLPYRIDINES AND THEIR USE IN THE TREATMENT OF CANCER<br/>[FR] SULFINYLPYRIDINES ET LEUR UTILISATION DANS LE TRAITEMENT DU CANCER
  申请人：OBLIQUE THERAPEUTICS AB

  公开号：WO2018146468A1

  公开（公告）日：2018-08-16

  There is provided compounds of formula I (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3, R4 and n have meanings provided in the description, which compounds are useful in the treatment of cancers.

  提供了式I（I）的化合物或其药用盐，其中L、R1、R2、R3、R4和n的含义如描述中所提供，这些化合物在治疗癌症方面是有用的。
• DISUBSTITUTED TRIFLUOROMETHYL PYRIMIDINONES AND THEIR USE
  申请人：BAYER PHARMA AKTIENGESELLSCHAFT

  公开号：US20160221965A1

  公开（公告）日：2016-08-04

  The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.

  本申请涉及新颖的2,5-二取代6-(三氟甲基)嘧啶-4(3H)-酮衍生物，其制备方法，其单独或与其他药物联合用于治疗和/或预防疾病，以及用于制备治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管、肾脏、炎症和纤维化疾病。
• PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
  申请人：Arora Nidhi

  公开号：US20120015962A1

  公开（公告）日：2012-01-19

  Compounds of the formula I or II: wherein X, m, Ar, R 1 and R 2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.

  式I或II的化合物： 其中X，m，Ar，R1和R2如本文所定义。所述化合物对于治疗IRAK介导的疾病是有用的。

表征谱图