Nalmefene

Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders[1][2][3][4].

Product Specifications

CAS Number

[55096-26-9]

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

Apoptosis; NF-κB; NO Synthase; Opioid Receptor; p38 MAPK; Reactive Oxygen Species (ROS) ; Toll-like Receptor (TLR)

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/nalmefene.html

Concentration

10mM

Purity

99.94

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC6CC6)CC4)C=CC(O)=C5O[C@@]3([H])C(CC1)=C

Molecular Formula

C21H25NO3

Molecular Weight

339.43

Precautions

H302, H312, H332

References & Citations

[1]Wang DS, et al. Nalmefene: a long-acting opioid antagonist. Clinical applications in emergency medicine. J Emerg Med. 1998 May-Jun;16 (3) :471-5.|[2]Osborn MD, et al. In vivo characterization of the opioid antagonist nalmefene in mice. Life Sci. 2010 Apr 10;86 (15-16) :624-30.|[3]Montesinos J, et al. Nalmefene Prevents Alcohol-Induced Neuroinflammation and Alcohol Drinking Preference in Adolescent Female Mice: Role of TLR4. Alcohol Clin Exp Res. 2017 Jul;41 (7) :1257-1270.|[4]Koga M, et al. Nalmefene, an opioid receptor modulator, aggravates atherosclerotic plaque formation in apolipoprotein E knockout mice by enhancing oxidized low-density lipoprotein uptake in macrophages. Biochem Biophys Rep. 2024 Mar 23;38:101688.