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

dc.contributor.author

Goldberg, Joel S

dc.coverage.spatial

United States

dc.date.accessioned

2015-07-31T15:44:42Z

dc.date.issued

2011

dc.description.abstract

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.

dc.identifier

http://www.ncbi.nlm.nih.gov/pubmed/21863129

dc.identifier

pmc-5-2011-019

dc.identifier.eissn

1177-391X

dc.identifier.uri

https://hdl.handle.net/10161/10355

dc.language

eng

dc.publisher

SAGE Publications

dc.relation.ispartof

Perspect Medicin Chem

dc.relation.isversionof

10.4137/PMC.S6803

dc.subject

analgesics

dc.subject

opioid peptided esters

dc.title

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

dc.type

Journal article

pubs.author-url

http://www.ncbi.nlm.nih.gov/pubmed/21863129

pubs.begin-page

19

pubs.end-page

26

pubs.organisational-group

Anesthesiology

pubs.organisational-group

Anesthesiology, VA Anesthesiology Service

pubs.organisational-group

Clinical Science Departments

pubs.organisational-group

Duke

pubs.organisational-group

School of Medicine

pubs.publication-status

Published

pubs.volume

5

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