16590-41-3

• 常用中文名：纳曲酮
• 常用英文名：naltrexone
• CAS号：16590-41-3
• 分子式：C₂₀H₂₃NO₄
• 分子量：341.40
• 相关类别： 原料药 专科用药 解毒药
• 发布时间：2018-03-24 08:00:00
• 更新时间：2024-01-05 12:20:23
• Naltrexone 是 Opioid receptor 的拮抗剂。Naltrexone 在体内抑制细胞增殖。Naltrexone 通过干扰细胞信号和改变免疫系统来抑制肿瘤生长。

名称

• 中文名: 纳曲酮
• 英文名: naltrexone
• 中文别名: 17-(环丙甲基)-4,5-环氧-3,14-二羟基吗啡烷-6-酮; 纳屈酮
• 英文别名: Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-, (5α)-; Trexonil; NeMexin; (1S,5R,13R,17S)-4-(Cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0.0.0]octadeca-7(18),8,10-trien-14-on; Depotrex; ReVia; en1939; Naltrel; en1639; Naltrexone; Vivitrol; (5α)-17-(Cyclopropylmethyl)-3,14-dihydroxy-4,5-epoxymorphinan-6-one; Antaxone; trexan; (1S,5R,13R,17S)-4-(cyclopropylmethyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0.0.0]octadeca-7(18),8,10-trien-14-one; (1S,5R,13R,17S)-4-(cyclopropylméthyl)-10,17-dihydroxy-12-oxa-4-azapentacyclo[9.6.1.0.0.0]octadéca-7(18),8,10-trién-14-one; celupan; En 1639A; Um-792; (5a)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one; Nalorex; Depade

物化性质

• 密度: 1.5±0.1 g/cm3
• 沸点: 558.1±50.0 °C at 760 mmHg
• 熔点: 168-170ºC
• 分子式: C₂₀H₂₃NO₄
• 分子量: 341.40
• 闪点: 291.4±30.1 °C
• 精确质量: 341.162720
• PSA: 70.00000
• LogP: 1.80
• 蒸汽压: 0.0±1.6 mmHg at 25°C
• 折射率: 1.709
• 储存条件: 库房通风低温干燥,与氧化剂,食品分开储运

生物活性

• 描述: Naltrexone 是 Opioid receptor 的拮抗剂。Naltrexone 在体内抑制细胞增殖。Naltrexone 通过干扰细胞信号和改变免疫系统来抑制肿瘤生长。
• 相关类别:
  研究领域 >> 癌症
  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
• 参考文献:

  [1]. Couto RD, et al. Low Doses Naltrexone: The Potential Benefit Effects for its Use in Patients with Cancer. Curr Drug Res Rev. 2021;13(2):86-89.

  [2]. Lobmaier PP, et al. Naltrexone depot formulations for opioid and alcohol dependence: a systematic review. CNS Neurosci Ther. 2011 Dec;17(6):629-36.

  [3]. Mannelli P, Peindl KS, Wu LT. Pharmacological enhancement of naltrexone treatment for opioid dependence: a review. Subst Abuse Rehabil. 2011 Jun;2011(2):113-123.

  [4]. Swift R, Oslin DW, Alexander M, Forman R. Adherence monitoring in naltrexone pharmacotherapy trials: a systematic review. J Stud Alcohol Drugs. 2011 Nov;72(6):1012-8.

  [5]. Makowski CT, Gwinn KM, Hurren KM. Naltrexone/bupropion: an investigational combination for weight loss and maintenance. Obes Facts. 2011;4(6):489-94.

  [6]. Hulse GK. Improving Clinical Outcomes for Naltrexone as a Management of Problem Alcohol Use. Br J Clin Pharmacol. 2012 Sep 5. doi: 10.1111/j.1365-2125.2012.04452.x.

  [7]. Naltrexone

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : QD2155000 CHEMICAL NAME : Morphinan-6-one, 17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy - CAS REGISTRY NUMBER : 16590-41-3 LAST UPDATED : 199806 DATA ITEMS CITED : 9 MOLECULAR FORMULA : C20-H23-N-O4 MOLECULAR WEIGHT : 341.44 WISWESSER LINE NOTATION : T B6566 B6/CO 4ABBC R BX FV HO PN GHT&&TTJ CQ JQ P1- AL3TJ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 551 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 1100 mg/kg SEX/DURATION : female 1-22 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - delayed effects TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 21 mg/kg SEX/DURATION : female 10-19 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Sex chromosome loss and nondisjunction MUTATION DATA TYPE OF TEST : Sister chromatid exchange TEST SYSTEM : Human Lymphocyte DOSE/DURATION : 1 gm/L REFERENCE : ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 1,180,1979

安全

• 符号: GHS02, GHS06, GHS08
• 信号词: Danger
• 危害声明: H225-H301 + H311 + H331-H370
• 警示性声明: P210-P260-P280-P301 + P310-P311
• 危害码 (欧洲): F,T
• 风险声明 (欧洲): 11-23/24/25-39/23/24/25
• 安全声明 (欧洲): 16-36/37-45
• 危险品运输编码: UN1230 - class 3 - PG 2 - Methanol, solution

合成路线

上下游产品

上游产品  9
1407490-23-6 52446-24-9 7051-34-5 16676-29-2
33522-95-1 1489-69-6 2516-33-8 16617-07-5
5911-08-0
下游产品  6
111555-53-4 55096-26-9 73232-52-7 105618-26-6
161532-22-5 16676-29-2