推荐产品
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
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
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
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
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
Psychopharmacology, 149(2), 115-120 (2000)
Pharmacologic Profile of Naloxegol, a Peripherally Acting mu-Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation
Journal of Pharmacology and Experimental Therapeutics, 361(2), 280-291 (2017)
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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