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Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics
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 an...
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Libertas Academica
2011
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3153123/ https://www.ncbi.nlm.nih.gov/pubmed/21863129 http://dx.doi.org/10.4137/PMC.S6803 |
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author | Goldberg, Joel S. |
author_facet | Goldberg, Joel S. |
author_sort | Goldberg, Joel S. |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-3153123 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | Libertas Academica |
record_format | MEDLINE/PubMed |
spelling | pubmed-31531232011-08-23 Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics Goldberg, Joel S. Perspect Medicin Chem Perspective 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. Libertas Academica 2011-07-25 /pmc/articles/PMC3153123/ /pubmed/21863129 http://dx.doi.org/10.4137/PMC.S6803 Text en © the author(s), publisher and licensee Libertas Academica Ltd. This is an open access article. Unrestricted non-commercial use is permitted provided the original work is properly cited. |
spellingShingle | Perspective Goldberg, Joel S. Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title | Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title_full | Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title_fullStr | Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title_full_unstemmed | Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title_short | Low Molecular Weight Opioid Peptide Esters Could be Developed as a New Class of Analgesics |
title_sort | low molecular weight opioid peptide esters could be developed as a new class of analgesics |
topic | Perspective |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3153123/ https://www.ncbi.nlm.nih.gov/pubmed/21863129 http://dx.doi.org/10.4137/PMC.S6803 |
work_keys_str_mv | AT goldbergjoels lowmolecularweightopioidpeptideesterscouldbedevelopedasanewclassofanalgesics |