Authors: Barry, U.; Zuo, Z.

Source: Current Pharmaceutical Design, Volume 11, Number 10, April 2005 , pp. 1343-1350(8)

Publisher: Bentham Science Publishers

Abstract:

Opioids are commonly used analgesics in clinical practice. Three opioid receptors (, and ) that mediate opioid effects have been identified by molecular cloning. Each type of opioid receptors consists of subtypes of receptors as suggested by pharmacological studies. Although opioid receptors are the major receptor to mediate the analgesic effects of opioids, and receptors are also important in anti-nociception (for example, and receptors can mediate spinal analgesia).

Recently, the cytoprotective effects of opioids have been recognized. The presence of opioids during harmful events such as ischemia reduces cell injury in multiple organs including heart and brain. These effects appear to be mediated by receptors in most studies. A new form of cytoprotection in which a prior exposure to opioids renders protection against cell ischemia (opioid preconditioning) has been identified. In the heart, this opioid preconditioning-induced protection has been well documented by multiple studies and may be mediated by ' receptors, Gi/o proteins, protein kinase C, ATPsensitive potassium channels and free radicals. Our initial study suggests that opioid preconditioning also induces neuroprotection. This neuroprotection involves 1 receptors, mitochondrial ATP-sensitive potassium channels and free radical production.

In this review, we will briefly describe the analgesic effects of opioids. We will focus our discussion on opioid preconditioning-induced protection and its mechanisms. Opioids and agents that specifically work on the signaling molecules for opioid preconditioning-induced protection may prove to be useful in inducing protection against ischemia in clinical practice.

Keywords: opioids; opioid receptors; analgesia; ischemia-reperfusion injury; cardioprotection; neuroprotection; preconditioning

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612053507459

Affiliations: 1: Department of Anesthesiology, University of Virginia Health System, 1 Hospital Drive, PO Box 800710, Charlottesville, Virginia 22908-0710, USA.

Publication date: 2005-04-01

More about this publication?

• Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.
  
  Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.

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