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Related Concept Videos

Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
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Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
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GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
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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.
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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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Measuring Caenorhabditis elegans Sensitivity to the Acetylcholine Receptor Agonist Levamisole
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Published on: June 7, 2022

Levamisole receptors: a second awakening.

Richard J Martin1, Alan P Robertson, Samuel K Buxton

  • 1Department of Biomedical Sciences, Iowa State University, Ames, IA 50011-1250, USA. rjmartin@iastate.edu

Trends in Parasitology
|May 22, 2012
PubMed
Summary

Levamisole and pyrantel activate nematode acetylcholine receptors to treat roundworm infections. New research reveals these receptors are plastic and form diverse subtypes, impacting anthelmintic drug effectiveness.

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Published on: December 30, 2012

Area of Science:

  • Veterinary pharmacology
  • Molecular parasitology
  • Drug discovery

Background:

  • Levamisole and pyrantel, developed in 1965, are established anthelmintics targeting nematode acetylcholine receptors.
  • These drugs are crucial for treating roundworm infections in both human and animal populations.
  • Recent advancements have revitalized interest in their mechanisms of action and resistance.

Purpose of the Study:

  • To explore the detailed modes of action and resistance of levamisole and pyrantel.
  • To investigate the plasticity and diversity of nematode acetylcholine receptors.
  • To understand how receptor subtypes influence sensitivity to cholinergic anthelmintics.

Main Methods:

  • Reconstitution of nematode acetylcholine receptors to enable detailed structural and functional analysis.
  • Comparative studies across different species to identify receptor subtype variations.
  • Pharmacological characterization of receptor-anthelmintic interactions.

Main Results:

  • Demonstrated that nematode acetylcholine receptors are plastic and can form diverse subtypes.
  • Identified species-dependent variations in receptor subtypes.
  • Showcased differential sensitivities of receptor subtypes to specific cholinergic anthelmintics.

Conclusions:

  • The plasticity of levamisole receptors leads to diverse subtypes with varying anthelmintic sensitivities.
  • Understanding these receptor dynamics is key to optimizing current treatments and developing new anthelmintics.
  • This knowledge is expected to guide research on other ion channel-targeting anthelmintics like ivermectin and emodepside.