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Related Concept Videos

Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
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,...
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...
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Adrenergic Agonists: Indirect-Acting Agents01:25

Adrenergic Agonists: Indirect-Acting Agents

Indirect-acting adrenergic agonists potentiate the effects of endogenous catecholamines through different mechanisms without directly binding to adrenoceptors.
One mechanism involves depleting stored catecholamines by displacing them from synaptic vesicles. These agents, known as "displacers," are transported into vesicles at the expense of noradrenaline. Examples include amphetamine and tyramine, which lack a catechol moiety, resulting in prolonged action, improved oral bioavailability, and...

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Latest advances in cannabinoid receptor agonists.

Ganesh A Thakur1, Ritesh Tichkule, Shama Bajaj

  • 1Northeastern University, Center for Drug Discovery, 116 Mugar Hall, Boston, MA 02115, USA. g.thakur@neu.edu

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Researchers reviewed recent patents for cannabinoid agonists, focusing on novel chemical scaffolds. The endocannabinoid system is a key target for treating various diseases.

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Area of Science:

  • Pharmacology
  • Medicinal Chemistry

Background:

  • The endocannabinoid system plays a crucial role in numerous pathophysiological processes.
  • It is a therapeutic target for neurodegenerative diseases, cancer, obesity, and pain.
  • Significant advancements have been made in developing selective and potent cannabinoid receptor ligands.

Purpose of the Study:

  • To review the latest developments in cannabinoid agonist research.
  • To summarize novel chemical scaffolds for CB-selective agonists disclosed in patents between January 2008 and June 2009.

Main Methods:

  • Literature search of PubMed for research articles and reviews.
  • Patent database searches including European patents (espacenet.com), SciFinder Scholar, and US patents (uspto.gov).

Main Results:

  • Patent activity is particularly high in the area of CB2 selective agonists.
  • Novel chemical scaffolds for cannabinoid agonists have been identified.

Conclusions:

  • Developing peripherally restricted CB1/CB2 agonists by limiting blood-brain barrier (BBB) penetrability is a key strategy.
  • Enhancing CB2-selectivity is crucial for avoiding adverse central CB1-mediated side effects.