Delta-Selective Glycopeptides Related to Enkephalin Produce Profound Analgesia with Reduced Side Effects in Mice
Abstract
The use of endogenous neuropeptides such as enkephalins and endorphins as drugs has remained an elusive goal since the 1970's. The principle reason for this is that peptides generally do not cross the blood-brain barrier, and are quickly degraded in the blood stream prior to delivery to opiate receptors in the brain. Animal research with glycosylated enkephalins and endorphins (dynorphins) indicates that potent analgesia is possible after intravenous or sub-cutaneous injection. Glycopeptides derived from delta-selective opioid agonists have 2-3X the potency of morphine, and lack many of the side effects associated with muagonists such as morphine. Morphine is still used on the battlefield for combat casualty care, and it is anticipated that further development of the glycopeptide analgesics will result in superior analgesics with greatly reduced side effects. Recent developments in this area are reported.
Document Details
- Document Type
- Technical Report
- Publication Date
- Sep 01, 2004
- Accession Number
- ADA444903
Entities
People
- Edward J. Bilsky
- Richard D. Egleton
- Robin Polt
Organizations
- University of Arizona