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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...
Opioid Receptors: Overview01:22

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...
Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
Glucagon-like Receptor Agonists01:24

Glucagon-like Receptor Agonists

Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Prodrugs01:30

Prodrugs

Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...

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Endomorphin derivatives with improved pharmacological properties.

Pegah Varamini1, Joanne T Blanchfield, Istvan Toth

  • 1School of Chemistry and Molecular Biosciences, The University of Queensland, Brisbane, QLD 4072, Australia.

Current Medicinal Chemistry
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Modified endogenous opioid peptides, endomorphins, offer potent pain relief with fewer side effects than traditional opioids. Strategies focus on improving their stability and delivery for clinical use in managing severe and neuropathic pain.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Medicinal Chemistry

Background:

  • Centrally acting opioids like morphine are primary treatments for severe pain but cause adverse effects (constipation, respiratory depression, dependence) and are ineffective for neuropathic pain.
  • Endomorphins (endomorphin-1 and -2) are endogenous opioid peptides demonstrating potent antinociception in preclinical models, with a potentially improved side effect profile compared to opioid alkaloids.
  • Native endomorphins face limitations for clinical use due to poor metabolic stability and restricted penetration of the gastrointestinal mucosa and blood-brain barrier.

Purpose of the Study:

  • To review strategies for overcoming the limitations of native endomorphins for clinical application.
  • To discuss the design and synthesis of endomorphin analogs with enhanced pharmacokinetic properties and reduced adverse effects.
  • To provide insight into the development of opioid peptides as improved analgesics.

Main Methods:

  • Review of literature on chemical modifications of endomorphins to enhance stability and barrier penetration.
  • Analysis of strategies including the development of locally or globally-restricted peptide analogs.
  • Consideration of peptidase inhibitors as a supplementary approach.

Main Results:

  • Numerous endomorphin analogs have been designed and synthesized to improve metabolic stability and barrier penetration.
  • Chemical modifications have yielded pharmacologically active analogs with potential for reduced adverse effects.
  • Strategies focus on overcoming the inherent drawbacks of small peptides for therapeutic use.

Conclusions:

  • Chemical modifications represent the primary strategy for developing clinically viable endomorphin analogs.
  • Developed endomorphin analogs show promise for improved pain management with a better side effect profile.
  • Further research into endomorphin analog development could lead to novel analgesic therapies.