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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
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...
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...
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,...
Signal Transduction: Overview01:26

Signal Transduction: Overview

Cells respond to many types of information, often through receptor proteins positioned on the membrane. They respond to chemical signals, such as hormones, neurotransmitters, and other signaling molecules, initiating a series of molecular reactions to produce an appropriate response. This is called signal transduction. Cells also coordinate different responses elicited by the same signaling molecule via mediators, allowing molecular cross-talk.
Typically, signal transduction involves three...

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Tobacco Hornworm as an Insect Model System for Cannabinoid Pre-clinical Studies
05:25

Tobacco Hornworm as an Insect Model System for Cannabinoid Pre-clinical Studies

Published on: December 29, 2021

Functionally selective cannabinoid receptor signalling: therapeutic implications and opportunities.

Barbara Bosier1, Giulio G Muccioli, Emmanuel Hermans

  • 1Unité de Chimie Pharmaceutique et de Radiopharmacie (CMFA 7340), Louvain Drug Research Institute, Brussels, Belgium.

Biochemical Pharmacology
|March 9, 2010
PubMed
Summary

Cannabinoid receptors (CB1 and CB2) activate diverse signaling pathways. Understanding ligand-specific signaling, like functional selectivity, is key for developing targeted cannabinoid therapeutics.

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Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents
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Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents

Published on: August 22, 2025

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Tobacco Hornworm as an Insect Model System for Cannabinoid Pre-clinical Studies
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Published on: December 29, 2021

Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents
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Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents

Published on: August 22, 2025

Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • Cannabinoid receptors (CB1 and CB2) are G protein-coupled receptors (GPCRs) involved in numerous physiological functions.
  • The endocannabinoid system's complexity arises from multiple ligands and signaling pathways, necessitating precise regulation.

Purpose of the Study:

  • To review diverse signaling pathways activated by cannabinoid receptors.
  • To discuss mechanisms ensuring specificity in functional responses to cannabinoid ligands.
  • To examine evidence for functional selectivity and protean agonism at cannabinoid receptors.

Main Methods:

  • Literature review of in vitro and in vivo studies on cannabinoid receptor signaling.
  • Analysis of receptor-G protein coupling specificity.
  • Evaluation of ligand-dependent signaling outcomes.

Main Results:

  • Cannabinoid receptors activate multiple signaling pathways, supporting complex physiological control.
  • Evidence supports functional selectivity and protean agonism, where distinct ligands trigger specific downstream effects.
  • Ligand- or constitutive activity-dependent receptor-G protein coupling explains mediator specificity.

Conclusions:

  • Cannabinoid signaling exhibits complexity and specificity, particularly in ligand-receptor interactions.
  • In vitro findings on specificity are increasingly supported by in vivo evidence.
  • Selective manipulation of cannabinoid signaling pathways holds promise for developing effective and safe therapeutics.