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Opioid Receptors: Overview01:22

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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, D-Pen5]-enkephalin or DPDPE for...
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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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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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CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its effects by...

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Cellular mechanisms underlying the interaction between cannabinoid and opioid system.

D Parolaro1, T Rubino, D Viganò

  • 1Department of Structural and Functional Biology and Center of Neuroscience, University of Insubria, Busto Arsizio (VA), Italy. daniela.parolaro@uninsubria.it

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Area of Science:

  • Neuropharmacology
  • Molecular Biology
  • Systems Biology

Background:

  • Functional interactions between opioid and cannabinoid systems are increasingly recognized.
  • Co-administration of cannabinoids and opioids shows therapeutic potential for pain, immune, and emotional disorders.
  • Widespread drug abuse involves combined cannabinoid and opioid use, yet cellular/molecular mechanisms remain under-explored.

Purpose of the Study:

  • To review the biochemical and molecular mechanisms underlying opioid and cannabinoid system interactions.
  • To explore potential therapeutic applications and challenges associated with combined cannabinoid-opioid use.

Main Methods:

  • Literature review of existing studies on opioid and cannabinoid interactions.
  • Analysis of proposed molecular and cellular mechanisms.
  • Comparison of interactions within the central nervous system and periphery.

Main Results:

  • Key interaction mechanisms include opioid peptide release by cannabinoids, endocannabinoid release by opioids, direct receptor-receptor interactions, and intracellular pathway crosstalk.
  • Interactions may differ in brain reward networks versus those controlling antinociception, emotion, and cognition.
  • Central nervous system and peripheral interactions may also vary.

Conclusions:

  • Understanding opioid-cannabinoid interactions is crucial for developing novel therapeutic strategies.
  • Further research into these molecular underpinnings could unlock new treatments for various conditions.
  • The distinct nature of these interactions in different systems warrants further investigation.