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Merck
CN

N7758

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
化学文摘社编号:
51481-60-8
分子量:
399.87
NACRES:
NA.77
PubChem Substance ID:
24278050
UNSPSC Code:
12352200
MDL number:
MFCD00150901
Beilstein/REAXYS Number:
6260807

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产品名称

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

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

SMILES string

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

InChI key

TXMZWEASFRBVKY-IOQDSZRYSA-N

assay

≥98% (TLC and titration)

form

powder

optical activity

[α]25/D −178.6°, c = 2.5 in H2O(lit.)

color

white to off-white

solubility

ethanol: 3.3 mg/mL
H2O: 50 mg/mL

storage temp.

2-8°C

Quality Level

200

Gene Information

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

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Disclaimer

光敏。

Application

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

Biochem/physiol Actions

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.

Features and Benefits

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.

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

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

target_organs

Respiratory system

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

法规信息

涉药品监管产品
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000486132
0000486134
0000486134
0000486132
0000467017

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Opiate withdrawal-induced place aversion lasts for up to 16 weeks
Stinus L, et al.
Psychopharmacology, 149(2), 115-120 (2000)
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)
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)
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
Trauma: Critical Care, 83-83 (2007)
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Product Information Sheet - N7758

Product Information Sheet

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