AI Article Synopsis
- Isolated organ models, particularly the small bowel, are useful for studying how opioids affect smooth muscle contraction in pharmacological and toxicological research.
- The study focused on testing the effects of opioids carfentanil, remifentanil, and U-48800, alongside their antagonists naloxone, nalmefene, and naltrexone, using a rat bowel model.
- Results showed that carfentanil was the most potent opioid, and naltrexone was the most effective antagonist, making this model a reliable method for studying opioid impacts without needing electrical stimulation.
Article Abstract
Isolated organ models are a versatile tool for pharmacological and toxicological research. Small bowel has been used to assess the inhibition of smooth muscle contraction by opioids. In the present study, we set out to establish a pharmacologically stimulated rat bowel model. The effects of carfentanil, remifentanil and the new synthetic opioid U-48800 and their respective antagonists naloxone, nalmefene and naltrexone were studied in a small bowel model in rats. The IC values of the tested opioids were as follows: carfentanil (IC = 0.02 µmol/L, CI 0.02-0.03 µmol/L) ≫ remifentanil (IC = 0.51 µmol/L, CI 0.40-0.66 µmol/L) ≫ U-48800 (IC = 1.36 µmol/L, CI 1.20-1.54 µmol/L). The administration of the opioid receptor antagonists naloxone, naltrexone and nalmefene led to progressive, parallel rightward shifts of the dose-response curves. Naltrexone was most potent in antagonizing the effects of U-48800, whereas naltrexone and nalmefene were most effective in antagonizing the effects of carfentanil. In summary, the current model seems to be a robust tool to study opioid effects in a small bowel model without the necessity of using electrical stimulation.
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| http://dx.doi.org/10.1016/j.toxlet.2023.05.010 | DOI Listing |
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