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Related Concept Videos

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...
Ligand-Gated Ion Channel Receptor: Gating Mechanism01:30

Ligand-Gated Ion Channel Receptor: Gating Mechanism

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...
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.
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Dose-Response Relationship: Selectivity and Specificity01:25

Dose-Response Relationship: Selectivity and Specificity

Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and β2-adrenergic receptors...
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

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Nondepolarizing (Competitive) Neuromuscular Blockers: Mechanism of Action01:17

Nondepolarizing (Competitive) Neuromuscular Blockers: Mechanism of Action

Nondepolarizing neuromuscular blockers induce paralysis by competitively blocking nicotinic acetylcholine receptors at the muscle end plate. Examples include pancuronium, mivacurium, vecuronium, and rocuronium. These quaternary ammonium derivatives are administered intravenously, are poorly absorbed, and are excreted via the kidneys.
Competitive antagonists prevent acetylcholine from binding to its receptor, inhibiting membrane depolarization. Without conformational changes or intrinsic...

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Related Experiment Video

Updated: Jun 8, 2026

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate
04:48

A High-throughput Calcium-flux Assay to Study NMDA-receptors with Sensitivity to Glycine/D-serine and Glutamate

Published on: July 10, 2018

Partial agonists and subunit selectivity at NMDA receptors.

Rune Risgaard1, Kasper B Hansen, Rasmus P Clausen

  • 1Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, Denmark.

Chemistry (Weinheim an Der Bergstrasse, Germany)
|October 15, 2010
PubMed
Summary
This summary is machine-generated.

Developing selective drugs for glutamate receptors, like N-methyl-D-aspartic acid (NMDA) receptors, is challenging but crucial for treating brain disorders. New scaffolds show promise in targeting specific NMDA receptor subtypes.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Glutamate is the primary excitatory neurotransmitter in the central nervous system (CNS).
  • Dysregulation of glutamate signaling is implicated in various CNS diseases.
  • Targeting specific glutamate receptor subtypes offers therapeutic potential.

Purpose of the Study:

  • To explore the development of subunit-selective ligands for glutamate receptors.
  • To address the challenge of achieving subtype selectivity, particularly for N-methyl-D-aspartic acid (NMDA) receptors.
  • To identify novel molecular scaffolds capable of differentiating between NMDA receptor subunits.

Main Methods:

  • Investigated the structural properties of NMDA receptor binding sites.
  • Synthesized and characterized novel chemical scaffolds.
  • Evaluated ligand binding and functional activity at different NMDA receptor subtypes.

Main Results:

  • Identified conserved regions within the NMDA receptor binding site that hinder selective ligand development.
  • Developed a few novel scaffolds demonstrating potential for subunit selectivity.
  • These scaffolds offer a promising starting point for designing subtype-specific NMDA receptor modulators.

Conclusions:

  • Achieving subunit selectivity for NMDA receptors is synthetically challenging due to conserved binding site architecture.
  • The identified scaffolds represent a significant advancement in the pursuit of selective NMDA receptor ligands.
  • Further development of these scaffolds could lead to novel therapeutics for CNS disorders.