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纳洛酮

纳洛酮用途

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。

纳洛酮名称

[ CAS 号 ]:
465-65-6

[ 中文名 ]:
纳洛酮

[ 英文名 ]:
Naloxone

[中文别名 ]:

[英文别名 ]:

[14C]-Naloxone
[3H]-Naloxone
Narcanti
Nalone
Naloxonum
EN 1530 base
Narcon
l-Naloxone
Narcan
n-Allylnoroxymorphone

纳洛酮生物活性

[ 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.

纳洛酮物理化学性质

[ 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

纳洛酮毒性和生态

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)

纳洛酮安全信息

[ 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) ]:
7-16-36/37-45

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol, solution

纳洛酮合成路线

详细合成路线

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纳洛酮文献

Morphine-induced internalization of the L83I mutant of the rat μ-opioid receptor.

Br. J. Pharmacol. 172(2) , 593-605, (2014)

Naturally occurring single-nucleotide polymorphisms (SNPs) within GPCRs can result in alterations in various pharmacological parameters. Understanding the regulation and function of endocytic traffick...

Sympathetic activity induced by naloxone-precipitated morphine withdrawal is blocked in genetically engineered mice lacking functional CRF1 receptor.

Toxicol. Appl. Pharmacol. 283(1) , 42-9, (2015)

There is large body evidence indicating that stress can lead to cardiovascular disease. However, the exact brain areas and the mechanisms involved remain to be revealed. Here, we performed a series of...

Involvement of neurotransmitters in the action of the nociceptin/orphanin FQ peptide-receptor system on passive avoidance learning in rats.

Neurochem. Res. 39(8) , 1477-83, (2014)

The nociceptin/orphanin FQ peptide (NOP) receptor and its endogenous ligand plays role in several physiologic functions of the central nervous system, including pain, locomotion, anxiety and depressio...

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纳洛酮