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Related Concept Videos

Analgesia and Pain Management01:25

Analgesia and Pain Management

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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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Opioid Receptors: Overview01:22

Opioid Receptors: Overview

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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,...
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Opioid Analgesics: Synthetic and Semisynthetic Opioids01:15

Opioid Analgesics: Synthetic and Semisynthetic Opioids

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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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Nociception01:44

Nociception

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Nociception—the ability to feel pain—is essential for an organism’s survival and overall well-being. Noxious stimuli such as piercing pain from a sharp object, heat from an open flame, or contact with corrosive chemicals are first detected by sensory receptors, called nociceptors, located on nerve endings. Nociceptors express ion channels that convert noxious stimuli into electrical signals. When these signals reach the brain via sensory neurons, they are perceived as pain.
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Opioid Analgesics: Morphine and Other Natural Cogeners01:20

Opioid Analgesics: Morphine and Other Natural Cogeners

239
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...
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Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

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Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
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Related Experiment Video

Updated: Jun 26, 2025

Development of Recombinant Proteins to Treat Chronic Pain
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Recent Developments in Sigma-2 Receptor Compounds for Pain.

Robert B Raffa1, Joseph V Pergolizzi2

  • 1Pharmacology and Therapeutics, Temple University, Philadelphia, USA.

Cureus
|May 9, 2024
PubMed
Summary
This summary is machine-generated.

Sigma-2 receptors (S2R) show promise for treating neuropathic pain, a condition with limited options. Further research is needed to develop S2R compounds for clinical trials.

Keywords:
analgesiadrug discoveryneuropathic pains2r subtypesigma receptorstmem97

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Drug Discovery

Background:

  • Sigma receptors, particularly sigma-1 receptor (S1R) and sigma-2 receptor (S2R) subtypes, are emerging as significant therapeutic targets.
  • Advances in molecular biology, computational methods, and preclinical testing have elucidated their potential.

Purpose of the Study:

  • To review recent findings on the analgesic activity of sigma-2 receptor compounds.
  • To highlight the therapeutic potential of S2R ligands for neuropathic pain management.

Main Methods:

  • Literature review of recent reports on S2R compounds.
  • Analysis of preclinical data demonstrating analgesic effects.
  • Assessment of molecular and computational studies.

Main Results:

  • Accumulating evidence from preclinical models indicates positive effects of S2R compounds.
  • These findings suggest potential clinical effectiveness for neuropathic pain conditions.
  • Current therapeutic options for neuropathic pain are limited, highlighting the need for novel treatments.

Conclusions:

  • Sigma-2 receptor compounds demonstrate significant potential for the development of novel analgesics.
  • Further research is crucial to identify and characterize compounds suitable for clinical trials in treating intractable neuropathic pain.