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Related Concept Videos

Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
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Opioid Receptors: Overview

Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2, D-Pen5]-enkephalin or DPDPE for...
Production of Pharmaceuticals01:30

Production of Pharmaceuticals

Industrial insulin production uses genetically engineered E. coli expressing a proinsulin gene controlled by a tryptophan promoter and containing a methionine linker for later cleavage. The cells also carry ampicillin resistance for selective growth. Seed cultures are stored at −80 °C and production begins by thawing a small amount to inoculate starter cultures, which are progressively scaled to a 50,000-L bioreactor. In the bioreactor, E. coli grow in nutrient-rich media under sterile, tightly...
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
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The Central Dogma01:20

The Central Dogma

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RNA is the Missing Link Between DNA and Proteins
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Related Experiment Video

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A Magnetic Separation-Assisted High-Speed Homogenization Method for Large-Scale Production of Endosome-Derived Vesicles
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A Magnetic Separation-Assisted High-Speed Homogenization Method for Large-Scale Production of Endosome-Derived Vesicles

Published on: January 26, 2024

Recent advances in endomorphin engineering.

Attila Keresztes1, Attila Borics, Géza Tóth

  • 1Institute of Biochemistry, Biological Research Center, Hungarian Academy of Sciences, Szeged, Hungary.

Chemmedchem
|May 22, 2010
PubMed
Summary

New peptide drugs called endomorphins show promise as effective pain relievers. These compounds target mu-opioid receptors and may offer an alternative to traditional opiates with fewer side effects.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Neuroscience

Background:

  • Millions suffer from acute and chronic pain globally, often treated with opiates like morphine.
  • Current opiate treatments have significant drawbacks, including tolerance, dependence, and respiratory depression.
  • There is a critical need for novel analgesics with improved safety profiles.

Purpose of the Study:

  • To review recent advancements in the development of endomorphin derivatives as potential opioid analgesics.
  • To explore the design, synthesis, and pharmacological properties of these peptide-based compounds.
  • To assess the potential of endomorphins as substitutes for traditional opiates in pain management.

Main Methods:

  • Literature review of studies on endomorphin derivatives over the past decade.

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  • Analysis of research on design, radiolabeling, and pharmacological characterization.
  • Examination of structure-activity relationships of endomorphin analogues.

    • Main Results:

    • Endomorphins exhibit excellent mu-opioid receptor binding and potent analgesic effects.
    • Modified endomorphin analogues demonstrate potential as effective pain therapeutics.
    • These derivatives may offer a reduced propensity for adverse side effects compared to conventional opiates.

    Conclusions:

    • Endomorphin derivatives represent a promising class of compounds for novel pain management strategies.
    • Further research into endomorphin analogues could lead to safer and more effective analgesics.
    • Peptide-based therapeutics offer a viable alternative to current opiate-based pain treatments.