Repinotan, a Selective 5-HT1A-R-Agonist, Antagonizes Morphine-Induced Ventilatory Depression in Anesthetized Rats
@article{Guenther2010RepinotanAS, title={Repinotan, a Selective 5-HT1A-R-Agonist, Antagonizes Morphine-Induced Ventilatory Depression in Anesthetized Rats}, author={Ulf Guenther and Hermann Wrigge and Nils Ulrich Theuerkauf and Michael Boettcher and Georg Wensing and Joerg Zinserling and Christian Putensen and Andreas Hoeft}, journal={Anesthesia \& Analgesia}, year={2010}, volume={111}, pages={901–907} }
BACKGROUND:Spontaneous breathing during mechanical ventilation improves arterial oxygenation and cardiovascular function, but is depressed by opioids during critical care. Opioid-induced ventilatory depression was shown to be counteracted in anesthetized rats by serotonin(1A)-receptor (5-HT1A-R)-agonist 8-OH-DPAT, which cannot be applied to humans. Repinotan hydrochloride is a selective 5-HT1A-R-agonist already investigated in humans, but the effects on ventilation and nociception are unknown…
19 Citations
Selective 5-HT1A-R-agonist Repinotan Prevents Remifentanil-induced Ventilatory Depression and Prolongs Antinociception
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Repinotan prevented remifentanil-induced ventilatory depression in spontaneously breathing, anesthetized rats and prolonged the profound antinociception after discontinuation of remifENTanil infusion.
5-HT1A Receptor Agonist Befiradol Reduces Fentanyl-induced Respiratory Depression, Analgesia, and Sedation in Rats
- Medicine, BiologyAnesthesiology
- 2015
The reversal of opioid-induced respiratory depression and sedation by befiradol in adult rats was robust, whereas involved mechanisms are unclear, however, there were adverse concomitant decreases in fentanyl-induced analgesia and altered baseline ventilation, nociception, and behavior.
Effects of cholinesterase inhibitors and serotonin-1A receptor agonists on morphine-induced ventilatory depression and antinociception in rats.
- Biology, MedicineEuropean journal of pharmacology
- 2013
Central administration of CXCR4 antagonist prevents the development of peripheral neuropathic pain and modulates the spinal expression of neuropeptides and pro-inflammatory cytokines in mice: 9AP1-9
- Biology, Medicine
- 2014
Repinotan, a selective 5-HT1A-R-agonist, antagonizes morphine-induced ventilatory depression in anesthetized rats, while analgesia was not impaired and the expected ef fect could have been uncovered using a study design wih preliminary established opioid-induced respiratory depression and an additional loss of awareness.
Activation of 5-HT1A receptors in the preBötzinger region has little impact on the respiratory pattern
- BiologyRespiratory Physiology & Neurobiology
- 2015
Dual mechanisms of opioid-induced respiratory depression in the inspiratory rhythm-generating network
- BiologyeLife
- 2021
It is concluded that hyperpolarization of MOR-expressing preBötC neurons alone does not phenocopy OIRD, and the effects of MOR activation are twofold: pre-inspiratory spiking is reduced and excitatory synaptic transmission is suppressed, thereby disrupting network-driven rhythmogenesis.
Dual mechanisms of opioid-induced respiratory depression in the inspiratory rhythm-generating network
- BiologybioRxiv
- 2021
It is concluded that hyperpolarization of MOR-expressing preBötC neurons alone does not phenocopy OIRD, and the effects of MOR activation are twofold: 1) pre-inspiratory spiking is reduced and 2) excitatory synaptic transmission is suppressed, thereby disrupting network-driven rhythmogenesis.
Averting Opioid-induced Respiratory Depression without Affecting Analgesia.
- Biology, MedicineAnesthesiology
- 2018
None of the experimental drugs are adequate for therapeutic use in opioid-induced respiratory depression and all need further study of efficacy and toxicity, but all do highlight potential mechanisms of action and possible templates for further study and development.
Opioid-induced respiratory depression in humans: a review of pharmacokinetic-pharmacodynamic modelling of reversal.
- Biology, MedicineBritish journal of anaesthesia
- 2019
Sources of Inspiration: A Neurophysiologic Framework for Understanding Anesthetic Effects on Ventilatory Control
- MedicineCurrent Anesthesiology Reports
- 2013
Until reliable means for reversing drug-induced Ventilatory depression are developed, prompt recognition of ventilatory insufficiency and initiation of resuscitative measures remain the keys to patient safety.
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