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Related Concept Videos

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...
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...
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids01:21

Chemotherapy-Induced Nausea and Vomiting: Cannabinoids

Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids01:24

CNS Stimulants: Cocaine, Amphetamines and Cannabinoids

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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Intracranial Pharmacotherapy and Pain Assays in Rodents
02:26

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Published on: April 9, 2019

Endocannabinoids: a unique opportunity to develop multitarget analgesics.

Sabatino Maione1, Barbara Costa, Vincenzo Di Marzo

  • 1Endocannabinoid Research Group, Department of Experimental Medicine - Division of Pharmacology 'L. Donatelli', Second University of Naples, Naples, Italy Department of Biotechnology and Bioscience, University of Milano-Bicocca, Milan, Italy Endocannabinoid Research Group, Institute of Biomolecular Chemistry - C.N.R., Pozzuoli, Italy.

Pain
|April 30, 2013
PubMed
Summary
This summary is machine-generated.

Cannabinoid research has accelerated, revealing the complex "endocannabinoidome." Natural compounds may offer safer, more effective treatments for chronic pain and inflammation by modulating this system.

Keywords:
Biennial review of pain 2013EndocannabinoidsPain

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • Cannabis use dates back millennia, with key cannabinoid discoveries in the 1960s and receptor/endocannabinoid identification in the 1990s.
  • Recent research highlights the endocannabinoid signaling system's complexity and role in physiological and pathological conditions, particularly pain.

Purpose of the Study:

  • To review the evolution of cannabinoid research and the concept of the "endocannabinoidome."
  • To explore the potential of multitarget drugs and natural compounds for therapeutic manipulation of the endocannabinoid system.

Main Methods:

  • Literature review of cannabinoid research history and discoveries.
  • Analysis of the endocannabinoidome concept and its implications for drug development.

Main Results:

  • The endocannabinoid system is more complex than initially thought, involving multiple mediators and targets.
  • Natural compounds may offer advantages over single-target drugs for modulating the endocannabinoidome.

Conclusions:

  • The complexity of the endocannabinoidome necessitates multitarget drug development or revisiting natural compounds.
  • Modulating the endocannabinoidome with natural compounds shows promise for safe and effective treatment of chronic pain and inflammation.