465-65-6

• 常用中文名：纳洛酮
• 常用英文名：Naloxone
• CAS号：465-65-6
• 分子式：C₁₉H₂₁NO₄
• 分子量：327.37
• 相关类别： 原料药 专科用药 解毒药
• 发布时间：2018-08-06 19:54:23
• 更新时间：2026-07-01 14:15:06
• Naloxone 是 Opioid receptor 的拮抗剂。Naloxone 可减轻阿片类药物过量引起的呼吸抑制。Naloxone 可能会引起肺水肿和心律失常。

名称

• 中文名: 纳洛酮
• 英文名: naloxone
• 中文别名: (5alpha)-3,14-二羟基-17-丙-2-烯-1-基-4,5-环氧吗啡烷-6-酮; 纳洛酮杂质C; 纳洛酮,(控制); 纳洛酮碱; 纳洛酮杂质F
• 英文别名: l-naloxone; Narcon; 1-n-allyl-14-hydroxynordihydromorphinone; 12-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4ah-8,9c-iminoethanophenanthro(4,5; bcd]furan-5(6h)-one; (4R,4aS,7aR,12bS)-4a,9-dihydroxy-3-prop-2-enyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one; C07252; 1-n-allyl-7,8-dihydro-14-hydroxynormorphinone; l-n-allyl-7,8-dihydro-14-hydroxynormorphinone; Naloxone, (controlled); 17-allyl-4,5alpha-oxy-3,14-dihydroxymorphinan-6-one; l-n-allyl-14-hydroxynordihydromorphinone; 12-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4ah-8,9c-iminoethanophenanthro(4; bcd)furanone; NALOXONE; Narcanti; 17-allyl-4,5alpha-oxy-3,14-dihydroxy-morphinan-6-on; n-allyl-noroxymorphone; Naloxone //BP; (4R)-6,10aβ-Dihydroxy-11-allyl-4α,5-oxy-10β,4aβ-iminoethano)-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-3-one; 17-allyl-4,5-alpha-oxy-3,14-dihydroxymorphinan-6-one; Methanol (test Naloxone, 1.0 mg/mL）; l-Naloxone; (5alpha)-3,14-Dihydroxy-17-prop-2-en-1-yl-4,5-oxymorphinan-6-one; Morphinan-6-one,4,5-oxy-3,14-dihydroxy-17-(2-propen-1-yl)-, (5a); 12-allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4ah-8,9c-iminoethanophenanthro[4,5; Naloxone (1.0 mg/mL in Methanol); 5-oxy-3,14-dihydroxy-17-(2-propenyl)-(5alpha)-morphinan-6-on; Nafoxone Hydrochloride; 17-Allyl-4,5α-oxy-3,14-dihydroxymorphinan-6-one; Morphinan-6-one, 4,5-oxy-3,14-dihydroxy-17-(2-propen-1-yl)-, (5α); Narcan; Normorphinone, N-allyl-7,8-dihydro-14-hydroxy- (7CI); 5-bcd)furanone; 9: PN: WO03037310 FIGURE: 4 claimed sequence; Naloxonum; Naloxone Base; (5α)-4,5-oxy-3,14-dihydroxy-17-(2-propen-1-yl)morphinan-6-one; Naloxone impurity; 12-Allyl-7,7a,8,9-tetrahydro-3,7a-dihydroxy-4aH-8,9c-iminoethanophenanthro[4,5-bcd]furan-5(6H)-one; Nalone; [14C]-Naloxone; [3H]-Naloxone; EN 1530 base; 4,5-alpha-oxy-3,14-dihydroxy-17-(2-propenyl)-morphinan-6-on; n-Allylnoroxymorphone; Naloxona; Morphinan-6-one, 4,5-oxy-3,14-dihydroxy-17-(2-propenyl)-, (5a)- (9CI); Morphinan-6-one, 17-allyl-4,5a-oxy-3,14-dihydroxy- (8CI); Naloxone solution; Naloxone API

物化性质

• 密度: 1.43 g/cm3
• 沸点: 532.8ºC at 760 mmHg
• 熔点: 184ºC
• 分子式: C₁₉H₂₁NO₄
• 分子量: 327.37
• 闪点: 276.1ºC
• 精确质量: 327.14700
• PSA: 70.00000
• LogP: 1.23930
• 外观性状: 白色至略灰白色粉末
• 储存条件: 2-8°C

生物活性

• 描述: Naloxone 是 Opioid receptor 的拮抗剂。Naloxone 可减轻阿片类药物过量引起的呼吸抑制。Naloxone 可能会引起肺水肿和心律失常。
• 相关类别:
  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
• 参考文献:

  [1]. van Dorp E, et al. Naloxone treatment in opioid addiction: the risks and benefits. Expert Opin Drug Saf. 2007 Mar;6(2):125-32.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : QD2260000 CHEMICAL NAME : Morphinan-6-one, 4,5-alpha-epoxy-3,14-dihydroxy-17-(2-propenyl)- CAS REGISTRY NUMBER : 465-65-6 LAST UPDATED : 199806 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C19-H21-N-O4 MOLECULAR WEIGHT : 327.41 WISWESSER LINE NOTATION : T B6566 B6/CO 4ABBC R BX FV HO PN GHT&&TTJ CQ JQ P2U1 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 : 260 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 : Subcutaneous DOSE : 30 mg/kg SEX/DURATION : female 16-20 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - gastrointestinal system Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Implant DOSE : 500 ug/kg SEX/DURATION : female 17-21 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Newborn - behavioral MUTATION DATA TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Human Cells - not otherwise specified DOSE/DURATION : 120 umol/L/24H REFERENCE : JJCREP Japanese Journal of Cancer Research. (Elsevier Science Pub. BV, POB 211, 1000 AE Amsterdam, Netherlands) V.76- 1985- Volume(issue)/page/year: 78,519,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4324 No. of Facilities: 14 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 306 (estimated) No. of Female Employees: 121 (estimated)

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): 7-16-36/37-45
• 危险品运输编码: UN1230 - class 3 - PG 2 - Methanol, solution

合成路线

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