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Related Concept Videos

Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
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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...
Modified-Release Drug Delivery Systems: Site-Targeted01:24

Modified-Release Drug Delivery Systems: Site-Targeted

Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
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...
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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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The Expanded Endocannabinoid System/Endocannabinoidome as a Potential Target for Treating Diabetes Mellitus.

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Targeting the endocannabinoid system: to enhance or reduce?

Vincenzo Di Marzo1

  • 1Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council (CNR), Via Campi Flegrei 34, 80078, Pozzuoli, Naples, Italy. vdimarzo@icmib.na.cnr.it

Nature Reviews. Drug Discovery
|May 1, 2008
PubMed
Summary

The endocannabinoid system

Area of Science:

  • Neuroscience
  • Pharmacology
  • Biochemistry

Background:

  • Endocannabinoid levels and functions shift during disease.
  • Endocannabinoid mediators can act as protective or dysregulated signals.
  • Understanding endocannabinoid complexity is crucial for therapeutic development.

Purpose of the Study:

  • To explore the therapeutic potential of modulating the endocannabinoid system.
  • To identify compounds targeting endocannabinoid pathways for various diseases.
  • To address the challenges of clinical translation for endocannabinoid-based therapies.

Main Methods:

  • Review of current research on endocannabinoid signaling.
  • Analysis of pathological changes in endocannabinoid levels.
  • Exploration of pharmacological strategies to modulate endocannabinoid activity.

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Main Results:

  • Discovery of compounds that modulate endocannabinoid lifespan and action.
  • Identification of potential therapeutic applications for pain, neurological, and metabolic disorders.
  • Recognition of the pleiotropic effects of endocannabinoids.

Conclusions:

  • Modulating the endocannabinoid system offers therapeutic promise for numerous conditions.
  • Careful patient selection and disease staging are essential for effective clinical application.
  • Further research is needed to harness the full therapeutic potential of endocannabinoid modulation.