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Published on: June 9, 2017
[Antiarrhythmic properties of opioid receptor agonists]
Abstract:
Data on the antiarrhythmic properties of opioid receptor (OR) agonists have been systematized. An analysis of published works which indicate that opioids increase cardiac tolerance to arrhythmogenic influences both in vivo and in vitro has been performed. For example, occupancy of central micro- and delta-OR and also ORL1 receptors increases cardiac tolerance to arrhythmogenic action epinephrine and aconitine. In contrast, activation of central kapa-OR exacerbates arrhythmogenic action epinephrine. Stimulation of peripheral delta2- and kappa1-OR decreases an incidence of arrhythmias induced coronary artery occlusion and reperfusion in vivo. Occupancy of peripheral micro-, kappa2-, delta1-OR and also ORL1 receptors has no effect on the cardiac tolerance to arrhythmogenic action of ischemia and reperfusion but increases cardiac electrical stability in rats with post-infarction cardiosclerosis. Authors suggest that opioids which unable penetrate to blood barrier may be used for therapy of arrhythmias.
Insights
Opioid receptor (OR) agonists show antiarrhythmic properties, enhancing cardiac tolerance to arrhythmias. Certain OR subtypes may offer therapeutic potential for treating heart rhythm disorders.
Area of Science:
- Pharmacology
- Cardiology
- Neuroscience
Background:
- Opioid receptors (OR) play a role in cardiovascular regulation.
- Previous studies suggest a link between opioid signaling and cardiac function.
Purpose of the Study:
- To systematize data on the antiarrhythmic properties of opioid receptor agonists.
- To analyze the effects of various opioid receptor subtypes on cardiac tolerance to arrhythmias.
Main Methods:
- Systematic review and analysis of published in vivo and in vitro studies.
- Investigation of central and peripheral opioid receptor activation effects.
Main Results:
- Activation of central micro-, delta-OR, and ORL1 receptors increased cardiac tolerance to arrhythmogenic agents.
- Activation of central kappa-OR exacerbated epinephrine-induced arrhythmias.
- Stimulation of peripheral delta2- and kappa1-OR reduced arrhythmias during coronary artery occlusion and reperfusion.
- Peripheral micro-, kappa2-, delta1-OR, and ORL1 receptors did not affect ischemia/reperfusion tolerance but improved electrical stability in post-infarction cardiosclerosis models.
Conclusions:
- Opioid receptor agonists exhibit significant antiarrhythmic effects.
- Specific opioid receptor subtypes demonstrate differential modulation of cardiac arrhythmias.
- Opioids that do not cross the blood-brain barrier may be promising therapeutic agents for arrhythmias.
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