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Merck
CN

N7758

Sigma-Aldrich

纳洛酮盐酸盐二水合物 盐酸盐 二水合物

≥98% (TLC and titration),  μ, κ, δ, and σ opioid receptor antagonist, powder

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关于此项目

经验公式（希尔记法）:
C19H21NO4 · HCl · 2H2O
CAS Number:
51481-60-8
分子量:
399.87
Beilstein:
6260807
MDL编号:
MFCD00150901
UNSPSC代码:
12352200
PubChem化学物质编号:
24278050
NACRES:
NA.77

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Product Name

纳洛酮盐酸盐二水合物 盐酸盐 二水合物, ≥98% (TLC and titration), powder

质量水平

200

方案

≥98% (TLC and titration)

表单

powder

旋光性

[α]25/D −178.6°, c = 2.5 in H2O(lit.)

颜色

white to off-white

溶解性

ethanol: 3.3 mg/mL
H2O: 50 mg/mL

储存温度

2-8°C

SMILES字符串

O.O.Cl.Oc1ccc2C[C@H]3N(CC[C@@]45[C@@H](Oc1c24)C(=O)CC[C@@]35O)CC=C

InChI

1S/C19H21NO4.ClH.2H2O/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11;;;/h2-4,14,17,21,23H,1,5-10H2;1H;2*1H2/t14-,17+,18+,19-;;;/m1.../s1

InChI key

TXMZWEASFRBVKY-IOQDSZRYSA-N

基因信息

human ... OPRD1(4985), OPRK1(4986), OPRM1(4988), OPRS1(10280)

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相关类别

应用

Naloxone hydrochloride dihydrate has been used in:
  • isotonic saline and injected subcutaneously into experimental rats to study its involvement with withdrawal syndrome in morphine-dependent rats
  • as opioid receptor antagonist to examine the role of the endogenous opioid system in infantile amnesia for contextual fear
  • as a reference neutral antagonist to define the maximum effect (Emax) of the system

生化/生理作用

Competitive antagonist for μ, κ, δ, and σ opioid receptors; blocks the action of σ-agonists at opioid sites. Naloxone′s antagonistic effect last for about 45 min and thus, requires repeated dosage. It results in critical side effects such as pulmonary edema.

特点和优势

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

免责声明

光敏。

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H315,H319,H335

危险分类

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves

法规信息

监管及禁止进口产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000467017
0000467016
0000463060
0000463060
0000467016

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Pharmacologic Profile of Naloxegol, a Peripherally Acting mu-Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation
Floettmann E, et al.
Journal of Pharmacology and Experimental Therapeutics, 361(2), 280-291 (2017)
Opiate withdrawal-induced place aversion lasts for up to 16 weeks
Stinus L, et al.
Psychopharmacology, 149(2), 115-120 (2000)
Jee Hyun Kim et al.
Learning & memory (Cold Spring Harbor, N.Y.), 16(3), 161-166 (2009-02-19)
Several recent studies report that neurotransmitters that are critically involved in extinction in adult rats are not important for extinction in young rats. Specifically, pretest injection of the gamma-aminobutryic acid (GABA) receptor inverse agonist FG7142 has no effect on extinction
Opioid receptors regulate retrieval of infant fear memories: Effects of naloxone on infantile amnesia.
Weber M, et al.
Behavioral Neuroscience, 120(3), 702-702 (2006)
Iris Bachmutsky et al.
eLife, 10 (2021-05-19)
Opioids are perhaps the most effective analgesics in medicine. However, between 1999 and 2018, over 400,000 people in the United States died from opioid overdose. Excessive opioids make breathing lethally slow and shallow, a side-effect called opioid-induced respiratory depression. This
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