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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), powder

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

质量水平

检测方案

≥98% (TLC and titration)

形式

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

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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.

注意

光敏。

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

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

靶器官

Respiratory system

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

分析证书(COA)

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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
A Fischer et al.
British journal of pharmacology, 127(3), 605-608 (1999-07-13)
The recently identified endogenous agonists on the mu-opioid-receptor (mu OR), endomorphin-1 (EM-1) and endomorphin-2 (EM-2), induce a concentration dependent inhibition of electrical field stimulation (EFS)-induced tachykinin-mediated contractions of the guinea-pig bronchus (ED50s < 10 nM for both compounds). Surprisingly, only
Opiate withdrawal-induced place aversion lasts for up to 16 weeks
Stinus L, et al.
Psychopharmacology, 149(2), 115-120 (2000)
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)
Lamees Alhassen et al.
Pharmaceuticals (Basel, Switzerland), 14(10) (2021-10-24)
The opioid epidemic was triggered by an overprescription of opioid analgesics. In the treatment of chronic pain, repeated opioid administrations are required which ultimately lead to tolerance, physical dependence, and addiction. A possible way to overcome this conundrum consists of

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