Related Experiment Video
Updated: Dec 23, 2025
03:43
Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents
Published on: August 22, 2025
294
Novel approaches and current challenges with targeting the endocannabinoid system
Paula Morales1, Nadine Jagerovic1
1Instituto de Química Médica, Consejo Superior de Investigaciones Científicas , Madrid, Spain.
Expert Opinion on Drug Discovery
|April 28, 2020
Summary
The endocannabinoid system shows therapeutic potential for various diseases. Novel molecular strategies targeting cannabinoid receptors offer improved clinical outcomes by addressing challenges like pharmacokinetics and side effects.
Area of Science:
- Pharmacology
- Neuroscience
- Molecular Biology
Background:
- The endocannabinoid system's role in diseases like cancer and neurological disorders is established.
- Cannabinoid receptor ligands and enzyme inhibitors are key therapeutic targets.
- Phytocannabinoids are already used for conditions such as neuropathic pain and epilepsy.
Purpose of the Study:
- To review emerging molecular approaches in cannabinoid pharmacology.
- To discuss the clinical potential of novel strategies targeting the endocannabinoid system.
Main Methods:
- Review of current literature on cannabinoid receptor modulation.
- Analysis of novel strategies beyond traditional orthosteric ligands.
- Discussion of pharmacokinetic and off-target effect challenges.
Main Results:
- Orthosteric ligands for CB1 and CB2 receptors are primary research focus.
- Allosteric and biased modulation represent emerging strategies.
- Controlled off-target effects can enhance therapeutic potential.
Conclusions:
- Novel molecular approaches are crucial for advancing cannabinoid therapeutics.
- Addressing pharmacokinetic and psychoactive challenges is key.
- Allosteric and biased modulation offer promising avenues for drug development.
Related Concept Videos
01:25Analgesia and Pain Management
1.4K
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...
1.4K
01:24CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
672
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...
672
01:21Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
596
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,...
Two synthetic agonists of THC,...
596
01:22Opioid Receptors: Overview
3.7K
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,...
3.7K
01:26Targets for Drug Action: Overview
9.8K
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...
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...
9.8K
01:30Ligand-Gated Ion Channel Receptor: Gating Mechanism
3.6K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
3.6K