Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics.


Journal Article

Low molecular weight opioid peptide esters (OPE) could become a class of analgesics with different side effect profiles than current opiates. OPE may have sufficient plasma stability to cross the blood brain barrier (BBB), undergo ester hydrolysis and produce analgesia. OPE of dipeptides, tyr-pro and tyr-gly conjugated to ethanol have a structure similar to the anesthestic agent, etomidate. Based upon the analgesic activity of dipeptide opioids, Lipinski's criteria, and permeability of select GABA esters to cross the BBB, opioid peptides (OP) conjugated to ethanol, cholesterol or 3-glucose are lead recommendations. Preliminary animal data suggests that tyr-pro-ethyl ester crosses the BBB and unexpectedly produces hyperalgesia. Currently, there are no approved OP analgesics available for clinical use. Clinical trials of good manufacturing practice OP administered to patients suffering from chronic pain with indwelling intrathecal pumps could resolve the issue that OP may be superior to opiates and may redirect research.

Full Text

Duke Authors

Cited Authors

  • Goldberg, JS

Published Date

  • 2011

Published In

Volume / Issue

  • 5 /

Start / End Page

  • 19 - 26

PubMed ID

  • 21863129

Pubmed Central ID

  • 21863129

Electronic International Standard Serial Number (EISSN)

  • 1177-391X

Digital Object Identifier (DOI)

  • 10.4137/PMC.S6803


  • eng

Conference Location

  • United States