所有图片(4)
About This Item
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
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质量水平
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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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。
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
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
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
Thibaut Laboute et al.
eLife, 9 (2020-02-01)
GPR88 is an orphan G protein-coupled receptor (GPCR) considered as a promising therapeutic target for neuropsychiatric disorders; its pharmacology, however, remains scarcely understood. Based on our previous report of increased delta opioid receptor activity in Gpr88 null mice, we investigated
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)
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
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