Enhanced Potency of Receptor-Selective Opioids After Acute Burn Injury

Bs, Silbert; Aw, Lipkowski; Ms, Cepeda; Sk, Szyfelbein; Pf, Osgood; Carr, DB

doi:10.1213/00000539-199110000-00011

Cited by 19 publications

(4 citation statements)

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“…The reason for down-regulation of MOR at the dorsal horn is unclear. Increased plasma opioids reported during the acute period of burn injury [15,21] may downregulate the receptor level. This decreased MOR expression was also suggested to be involved in the development of hyperalgesia due to the decrease in the inhibitory regulation of nociceptive neurotransmission preand post-synaptically in the burn model.…”

Section: Discussionmentioning

confidence: 99%

Foot Hyperalgesia after Thoracic Burn Injury. Histochemical, Behavioral and Pharmacological Studies.

Ueda

Hirose

Takei

et al. 2001

Acta Histochem. Cytochem

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Using behavioral, immunohistochemical and pharmacological studies, we report here that large thoracic burn injuries remotely induce hindpaw hyperalgesia during the healing stage. During 2-3 weeks after thoracic burn injury when the skin was regenerating from the wound, we observed by formalin test that the number of flinching behaviors significantly increased and simultaneously we observed by von Frey test that rats developed mechano-hyperalgesia in the foot. In the dorsal horn of the lumbar spinal cord in burn injured rats, c-Fos expression was significantly augmented after plantar formalin injection. The expression of m-opioid receptor in burn injured rats was significantly decreased compared with that in sham operated rats. The expression of substance P and CGRP in the lumbar dorsal horn was not different between burn and sham operated animals. We also observed that intrathecal administration of glutamate receptor antagonists (MK801 and CNQX) but not cyclooxigenase-2 antagonist (NS-398) reversed the threshold of von Frey test on the foot up to the control level at 2 weeks after injury. Collectively, we analyzed a new pain model showing foot hyperalgesia after thoracic burn injury and demonstrated that neurotransmission of glutamate was enhanced at the lumbar spinal cord level by immunocytochemistry and intrathecal administration of NMDA and non NMDA antagonists. Although the precise mechanism of how remote hyperalgesia at the healing stage developed in this model remains to be confirmed, substances such as trophic factors released from the regenerating skin may cause systemic hyperalgesia including in the foot.

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Section: Discussionmentioning

confidence: 99%

Foot Hyperalgesia after Thoracic Burn Injury. Histochemical, Behavioral and Pharmacological Studies.

Ueda

Hirose

Takei

et al. 2001

Acta Histochem. Cytochem

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“…The analgesic activity of biphalin was also tested after an acute burn injury ( Table 4 ) [ 49 ]. The drugs morphine (a predominantly MOR agonist), biphalin (a predominantly MOR and DOR agonist), and U50,488H (a predominantly KOR agonist) were administered intravenously.…”

Section: Biphalin As An Analgesic Agent (In Vivo Studies)mentioning

confidence: 99%

Biphalin—A Potent Opioid Agonist—As a Panacea for Opioid System-Dependent Pathophysiological Diseases?

Redkiewicz

Dyniewicz

Misicka

2021

IJMS

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Biphalin, one of the opioid agonists, is a dimeric analog of enkephalin with a high affinity for opioid receptors. Opioid receptors are widespread in the central nervous system and in peripheral neuronal and non-neuronal tissues. Hence, these receptors and their agonists, which play an important role in pain blocking, may also be involved in the regulation of other physiological functions. Biphalin was designed and synthesized in 1982 by Lipkowski as an analgesic peptide. Extensive further research in various laboratories on the antinociceptive effects of biphalin has shown its excellent properties. It has been demonstrated that biphalin exhibits an analgesic effect in acute, neuropathic, and chronic animal pain models, and is 1000 times more potent than morphine when administered intrathecally. In the course of the broad conducted research devoted primarily to the antinociceptive effect of this compound, it has been found that biphalin may also potentially participate in the regulation of other opioid system-dependent functions. Nearly 40 years of research on the properties of biphalin have shown that it may play a beneficial role as an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent, and may also affect many physiological functions. This integral review analyzes the literature on the multidirectional biological effects of biphalin and its potential in the treatment of many opioid system-dependent pathophysiological diseases.

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“…Despite the enhanced potency of opioids after acute burn injury, 475 opioid requirements can be quite high. Burns cause substantial changes in metabolism and protein binding, but the pharmacokinetics of IV opioids remains unaltered.…”

Section: Opioids In Patients With Burn Injurymentioning

confidence: 99%