72782-05-9
Chemical Structure
β-Funaltrexamine
Synonym(s): β-FNA
- CAS No.: 72782-05-9
- Formula:C25H30N2O6
- Molecular Weight:454.52
InChIKey: PQKHESYTSKMWFP-WZJCLRDWSA-N
SMILES: O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])[C@@H](CC1)NC(/C=C/C(OC)=O)=O
Biological Activity: β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases[1][2][3][4].
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β-Funaltrexamine | β-Funaltrexamine (β-FNA) is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases. | |||||||||||||||||||||
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- [1]. Wu CC, et al. β-Funaltrexamine Displayed Anti-inflammatory and Neuroprotective Effects in Cells and Rat Model of Stroke. Int J Mol Sci. 2020;21(11):3866. Published 2020 May 29. [Content Brief]
- [2]. Davis RL, et al. The opioid antagonist, β-funaltrexamine, inhibits NF-κB signaling and chemokine expression in human astrocytes and in mice. Eur J Pharmacol. 2015;762:193-201. [Content Brief]
- [3]. Davis RL, et al. The opioid antagonist, β-funaltrexamine, inhibits lipopolysaccharide-induced neuroinflammation and reduces sickness behavior in mice. Physiol Behav. 2017;173:52-60. [Content Brief]
- [4]. Craig W Stevens, et al. The selective mu opioid antagonist β-funaltrexamine (β-FNA) reduces toll-like receptor-4 signaling.The FASEB Journal. 2010, April. 24 (S1):p.583.4.
Keywords
