AI Article Synopsis
- Morphine and other opiate alkaloids are commonly used to manage severe and chronic pain, but they come with side effects and limitations for certain pain types, like neuropathic pain from cancer.
- There’s a growing interest in developing modified versions of natural opioid peptides called endomorphin-1 and endomorphin-2 to enhance pain relief while minimizing drawbacks.
- This review highlights methods for creating stable peptidomimetics of these endomorphins and improving their effectiveness and absorption in the body, showing promising results for pain relief.
Article Abstract
Morphine and the other alkaloids found in the opium poppy plant still represent the preferred therapeutic tools to treat severe pain in first aid protocols, as well as chronic pain. The use of the opiate alkaloids is accompanied by several unwanted side effects; additionally, some forms of pain are resistant to standard treatments (e.g. neuropathic pain from cancer). For these reasons, there is currently renewed interest in the design and assay of modified versions of the potent endogenous opioid peptides endomorphin-1 and endomorphin-2. This review presents a selection of the strategies directed at preparing highly stable peptidomimetics of the endomorphins, and of the strategies aimed at improving central nervous system bioavailability, for which increased in vivo antinociceptive efficacy was clearly demonstrated.
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| http://dx.doi.org/10.2174/1568026615666150817103635 | DOI Listing |
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