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纳曲酮

纳曲酮用途

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。

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纳曲酮名称

[ CAS 号 ]:
16590-41-3

[ 中文名 ]:
纳曲酮

[ 英文名 ]:
naltrexone

[中文别名 ]:

纳屈酮

[英文别名 ]:

Trexonil
NeMexin
Depotrex
ReVia
en1939
Naltrel
en1639
Naltrexone
Vivitrol
Antaxone

纳曲酮生物活性

[ 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

纳曲酮物理化学性质

[ 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

纳曲酮毒性和生态

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

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纳曲酮安全信息

[ 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

纳曲酮合成路线

详细合成路线

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纳曲酮文献

Novel orally available salvinorin A analog PR-38 inhibits gastrointestinal motility and reduces abdominal pain in mouse models mimicking irritable bowel syndrome.

J. Pharmacol. Exp. Ther. 350(1) , 69-78, (2014)

The opioid and cannabinoid systems play a crucial role in multiple physiological processes in the central nervous system and in the periphery. Selective opioid as well as cannabinoid (CB) receptor ago...

Desensitization of functional µ-opioid receptors increases agonist off-rate.

Mol. Pharmacol. 86(1) , 52-61, (2014)

Desensitization of µ-opioid receptors (MORs) develops over 5-15 minutes after the application of some, but not all, opioid agonists and lasts for tens of minutes after agonist removal. The decrease in...

Treatment of alcohol dependence: recent progress and reduction of consumption.

Minerva Med. 105(6) , 447-66, (2014)

Alcohol dependence (AD) is a major public health problem. Currently, three drugs for the treatment of AD have been approved by both the European Medicines Agency (EMA) and the Food and Drug Administra...

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纳曲酮