Related Experiment Video
Updated: Feb 6, 2026
09:18
Time-resolved ElectroSpray Ionization Hydrogen-deuterium Exchange Mass Spectrometry for Studying Protein Structure and Dynamics
Published on: April 17, 2017
10.3K
NOP receptor pharmacological profile - A dynamic mass redistribution study
Davide Malfacini1,2, Katharina Simon1, Claudio Trapella3
1Molecular, Cellular and Pharmacobiology Section, Institute for Pharmaceutical Biology, University of Bonn, Bonn, Germany.
Plos One
|August 31, 2018
Summary
Label-free dynamic mass redistribution (DMR) successfully characterized NOP receptor ligands, revealing their pharmacological profiles. This method offers a holistic approach for studying G protein-coupled receptors and novel ligands.
Area of Science:
- Pharmacology
- Biochemistry
- Cellular Biology
Background:
- The Nociceptin/Orphanin FQ (N/OFQ) peptide NOP receptor is a G protein-coupled receptor (GPCR) linked to Gi/o proteins.
- Activation of NOP receptors influences cAMP production, calcium channels, and potassium currents.
Purpose of the Study:
- To systematically characterize the pharmacology of a diverse panel of NOP receptor ligands using label-free dynamic mass redistribution (DMR).
- To evaluate the utility of DMR technology for assessing GPCR ligand profiles.
Main Methods:
- Utilized label-free dynamic mass redistribution (DMR) technology.
- Employed Chinese hamster ovary (CHO) cells stably expressing the human NOP receptor.
- Assessed a range of peptide and non-peptide NOP receptor ligands with varying efficacies.
Main Results:
- DMR provided rank orders of potency for full and partial agonists and apparent affinities for antagonists.
- The pharmacological profiles obtained via DMR were comparable, yet not identical, to literature values from canonical assays.
- Demonstrated the successful application of DMR for comprehensive NOP receptor ligand characterization.
Conclusions:
- Label-free DMR is a robust method for investigating NOP receptor pharmacology.
- DMR technology effectively characterizes the cellular effects of novel NOP receptor ligands.
- This approach provides a holistic view of GPCR ligand interactions.
Related Concept Videos
01:22Adrenergic Antagonists: Pharmacological Actions of ɑ-Receptor Blockers
1.6K
α-Adrenergic antagonists, known as α-blockers, exert their effects by inhibiting α-adrenoceptors, leading to specific physiological actions. α1-blockers and α2-blockers have distinct pharmacological actions and therapeutic applications.
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...
α1-blockers: These drugs inhibit α1-adrenoceptors on smooth muscle cells, resulting in vasodilation. This vasodilation lowers blood pressure, making α1-blockers valuable in treating hypertension. Additionally,...
1.6K
01:27Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers
1.8K
β-receptor blockers significantly impact the cardiovascular system by counteracting catecholamine-induced sympathetic responses. These medications decrease heart rate, contractility, and cardiac output, potentially leading to cardiac depression, life-threatening bradycardia, and death. Therapeutically, β-blockers function as mild antihypertensives and are utilized in treating angina pectoris and cardiac arrhythmias. However, nonselective β-blockers inhibit β2-receptors in...
1.8K
01:31Internal Receptors
74.7K
Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
74.7K
01:52Atomic Mass
70.3K
Atoms — and the protons, neutrons, and electrons that compose them — are extremely small. For example, a carbon atom weighs less than 2 × 10−23 g. When describing the properties of tiny objects such as atoms, we use appropriately small units of measure, such as the atomic mass unit (amu). The amu was originally defined based on hydrogen, the lightest element, then later in terms of oxygen. Since 1961, it has been defined with regard to the most abundant isotope of carbon, atoms of which...
70.3K
01:25Blood Studies for Cardiovascular System III: Serum Lipid Profile
637
Understanding serum lipids is crucial for maintaining cardiovascular health and preventing heart disease and stroke.
Serum lipids are fats and fatty substances in the blood and are crucial for various bodily functions, including energy storage, cellular structure, and hormone production. Serum lipids consist of cholesterol, triglycerides, and phospholipids.
Cholesterol is a soft, fat-like substance found in all body cells. It is crucial for producing hormones, vitamin D, and substances that aid...
Serum lipids are fats and fatty substances in the blood and are crucial for various bodily functions, including energy storage, cellular structure, and hormone production. Serum lipids consist of cholesterol, triglycerides, and phospholipids.
Cholesterol is a soft, fat-like substance found in all body cells. It is crucial for producing hormones, vitamin D, and substances that aid...
637
01:54Molar Mass
86.9K
The identity of a substance is defined not only by the types of atoms or ions it contains but by the quantity of each type of atom or ion. For example, water, H2O, and hydrogen peroxide, H2O2, are alike in that their respective molecules are composed of hydrogen and oxygen atoms. However, because a hydrogen peroxide molecule contains two oxygen atoms, as opposed to the water molecule, which has only one, the two substances exhibit very different properties.
86.9K