Journal
CURRENT TOPICS IN MEDICINAL CHEMISTRY
Volume 16, Issue 2, Pages 141-155Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1568026615666150817103635
Keywords
Blood brain barrier; Endomorphins; Enzymatic stability; Lipophilicity; Opioid; Peptidomimetic
Categories
Funding
- Fondazione Umberto Veronesi
Ask authors/readers for more resources
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.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available