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Related Concept Videos

Principles of Drug Action01:24

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
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...
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.
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...
Drugs Affecting Neurotransmitter Synthesis01:29

Drugs Affecting Neurotransmitter Synthesis

Drugs affecting neurotransmitter synthesis can impact the adrenergic neuron and the synthesis of neurotransmitters. For example, α-methyltyrosine and carbidopa target specific enzymes involved in catecholamine synthesis. α-methyltyrosine inhibits the enzyme tyrosine hydroxylase, which converts tyrosine into dopamine. By blocking this enzyme, α-methyltyrosine reduces dopamine production and other catecholamines. Carbidopa, on the other hand, inhibits the enzyme dopa decarboxylase, which converts...
Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...

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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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FAAH Modulators from Natural Sources: A Collection of New Potential Drugs.

Catalin Nicoara1, Filomena Fezza2, Mauro Maccarrone1,3

  • 1Department of Biotechnological and Applied Clinical Sciences, University of L'Aquila, Via Vetoio, Coppito, 67100 L'Aquila, Italy.

Cells
|April 11, 2025
PubMed
Summary

Natural compounds can inhibit fatty acid amide hydrolase (FAAH), an enzyme that breaks down anandamide in the endocannabinoid system (ECS). This offers a safer therapeutic approach for various conditions.

Keywords:
FAAHcannabinoidsendocannabinoid systeminhibitorsnatural compounds

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • The endocannabinoid system (ECS) is vital for maintaining homeostasis, regulating immune responses, metabolism, and cognitive functions.
  • The ECS comprises endocannabinoids, cannabinoid receptors, and enzymes, and is implicated in various pathological conditions.
  • Modulating the ECS, particularly by inhibiting fatty acid amide hydrolase (FAAH), is a promising therapeutic strategy.

Purpose of the Study:

  • To explore the potential of natural substances as inhibitors of fatty acid amide hydrolase (FAAH).
  • To evaluate natural compounds as safer alternatives to synthetic inhibitors for therapeutic applications targeting the endocannabinoid system (ECS).

Main Methods:

  • Review of current research on natural compounds and their interaction with the endocannabinoid system (ECS).
  • Focus on the inhibition of fatty acid amide hydrolase (FAAH) by plant-derived compounds.
  • Analysis of the structural diversity and bioactivity of natural FAAH inhibitors.

Main Results:

  • Natural substances, including phytocannabinoids, flavonoids, and flavolignans, demonstrate efficient inhibition of FAAH.
  • These natural compounds offer a potentially lower toxicity profile compared to synthetic inhibitors.
  • The structural variety of natural inhibitors presents a valuable alternative for pharmacological development.

Conclusions:

  • Natural FAAH inhibitors represent a promising area for pharmacological research.
  • Plant-derived compounds provide a safer and diverse alternative to synthetic agents for modulating the endocannabinoid system (ECS).
  • Further development of natural inhibitors could lead to innovative therapeutic tools.