Abstract
Opioids have long been thought to act exclusively within the central nervous system. An increasing number of studies recently reported the existence of opioid receptors outside the central nervous system and therefore suggested that opioids are also able to produce analgesic effects in the periphery. Such effects are particularly prominent under painful inflammatory conditions, both in animals and in humans. During inflammatory processes, opioid receptors are transported from dorsal root ganglia towards the peripheral sensory nerve endings. At the same time, immune cells containing endogenous opioid peptides accumulate within the inflamed tissue. Environmental stimuli (e.g. stress) as well as releasing agents (e.g. corticotropin releasing factor, cytokines) can liberate these opioid peptides to interact with the neuronal opioid receptors and elicit local analgesia. The inflammation-induced activation of opioid production and the release of endogenous opioids from immune cells may lead to novel approaches for the development of peripherally acting analgesics. Clinical investigation now focuses on the development of new peripheral opioid agonists as well as on ways to stimulate the endogenous analgesic system in order to induce effective peripheral analgesia with reduced central side effects typically associated with opioids.
Keywords: peripheral opioid analgesia, inflammation, exogenous analgesia, endogenous analgesia, nociceptin/orl system, endomorphins, immune modulation of pain
Current Pharmaceutical Biotechnology
Title: Peripheral Opioid Analgesia
Volume: 4 Issue: 4
Author(s): W. Janson and C. Stein
Affiliation:
Keywords: peripheral opioid analgesia, inflammation, exogenous analgesia, endogenous analgesia, nociceptin/orl system, endomorphins, immune modulation of pain
Abstract: Opioids have long been thought to act exclusively within the central nervous system. An increasing number of studies recently reported the existence of opioid receptors outside the central nervous system and therefore suggested that opioids are also able to produce analgesic effects in the periphery. Such effects are particularly prominent under painful inflammatory conditions, both in animals and in humans. During inflammatory processes, opioid receptors are transported from dorsal root ganglia towards the peripheral sensory nerve endings. At the same time, immune cells containing endogenous opioid peptides accumulate within the inflamed tissue. Environmental stimuli (e.g. stress) as well as releasing agents (e.g. corticotropin releasing factor, cytokines) can liberate these opioid peptides to interact with the neuronal opioid receptors and elicit local analgesia. The inflammation-induced activation of opioid production and the release of endogenous opioids from immune cells may lead to novel approaches for the development of peripherally acting analgesics. Clinical investigation now focuses on the development of new peripheral opioid agonists as well as on ways to stimulate the endogenous analgesic system in order to induce effective peripheral analgesia with reduced central side effects typically associated with opioids.
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Cite this article as:
Janson W. and Stein C., Peripheral Opioid Analgesia, Current Pharmaceutical Biotechnology 2003; 4 (4) . https://dx.doi.org/10.2174/1389201033489766
DOI https://dx.doi.org/10.2174/1389201033489766 |
Print ISSN 1389-2010 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4316 |
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