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Updated: Oct 21, 2025
Magnetic Isolation of Microglial Cells from Neonate Mouse for Primary Cell Cultures
Published on: July 25, 2022
Effects of remifentanil on human C20 microglial pro-inflammatory activation
N Cappoli1, P Aceto, E Tabolacci
1Università Cattolica del Sacro Cuore, Dipartimento di Sicurezza e Bioetica, Sezione di Farmacologia, Rome, Italy. paola.aceto@policlinicogemelli.it.
Objective:
Remifentanil (RF) is a potent short-acting μ-opioid receptor agonist. Although preferred for its unique pharmacokinetics, the clinical use may be limited by hyperalgesia. Preclinical studies have shown a potential role of microglia on the development of hyperalgesia, with limited and conflicting evidence on RF. Considering the role of microglia in the initiation and maintenance of brain inflammation and their different responses among species, we aimed at characterizing RF effects on human adult microglia in vitro.
Materials And Methods:
RF was tested at clinically relevant concentrations on the human microglial C20 cell line. Expression and release of interleukin-6 (IL-6) and brain derived neurotrophic factor (BDNF) were assessed under basal and inflammatory conditions.
Results:
The expression and secretion of IL-6 significantly increased in C20 cells in response to pro-inflammatory cytokines. RF did not modify this response neither under basal nor under inflammatory conditions. No toxicity due to RF was detected. The drug displayed a modest stimulatory effect on the production of BDNF.
Conclusions:
Although RF does not exert direct pro-inflammatory actions on human adult microglia, its effects on BDNF, a crucial mediator of pain transmission, suggest a possible role on neuroinflammation and pain perception.
Insights
Remifentanil (RF) does not directly increase inflammation in human microglia. However, it may influence pain perception by affecting brain-derived neurotrophic factor (BDNF).
Area of Science:
- Neuroscience
- Pharmacology
- Immunology
Background:
- Remifentanil (RF) is a short-acting opioid agonist with unique pharmacokinetics.
- Clinical use of RF may be limited by hyperalgesia, potentially involving microglia.
- Evidence on RF's effect on microglia and hyperalgesia is limited and conflicting.
Purpose of the Study:
- To characterize the effects of RF on human adult microglia in vitro.
- To investigate RF's impact on pro-inflammatory cytokine release and BDNF production.
- To assess RF's potential role in neuroinflammation and pain perception.
Main Methods:
- Human microglial C20 cell line was treated with clinically relevant concentrations of RF.
- Expression and release of IL-6 and BDNF were measured under basal and inflammatory conditions.
- Cell viability was assessed to detect any RF-induced toxicity.
Main Results:
- Pro-inflammatory cytokines significantly increased IL-6 expression and secretion in C20 cells.
- RF did not alter IL-6 response under basal or inflammatory conditions.
- RF showed a modest stimulatory effect on BDNF production without causing toxicity.
Conclusions:
- RF does not exhibit direct pro-inflammatory effects on human microglia.
- RF's influence on BDNF suggests a potential role in neuroinflammation and pain.
- Further research is needed to elucidate RF's precise mechanisms in pain perception.
