Related Experiment Video
Updated: Apr 14, 2026
07:25
Identification of Dopamine D1-Alpha Receptor Within Rodent Nucleus Accumbens by an Innovative RNA In Situ Detection Technology
Published on: March 27, 2018
9.1K
Structural basis for Na(+)-sensitivity in dopamine D2 and D3 receptors
Mayako Michino1, R Benjamin Free, Trevor B Doyle
1Department of Physiology and Biophysics, Weill Medical College of Cornell University, New York, NY, USA. les2007@med.cornell.edu.
Chemical Communications (Cambridge, England)
|April 22, 2015
Summary
Sodium ions (Na(+)) critically influence dopamine D2-like receptor binding. Computational analysis revealed key interactions mediating Na(+) effects on receptor structure and ligand binding, expanding understanding of receptor pharmacology.
Area of Science:
- Neuroscience
- Pharmacology
- Structural Biology
Background:
- Dopamine receptors are crucial drug targets.
- Sodium ions are known to modulate G protein-coupled receptor (GPCR) function.
- The specific role of sodium in dopamine D2-like receptor ligand binding remains incompletely understood.
Purpose of the Study:
- To elucidate the structural mechanisms underlying sodium ion sensitivity in dopamine D2-like receptor ligand binding.
- To identify specific molecular interactions responsible for sodium's influence on receptor conformation and ligand affinity.
Main Methods:
- Computational analysis, including molecular modeling and simulations.
- In vitro binding assays to validate computational findings.
Main Results:
- Identified critical interactions mediating the propagation of sodium ion effects.
- Demonstrated how sodium ions alter receptor conformations.
- Revealed the impact of sodium on the ligand-binding site.
Conclusions:
- Sodium ions play a significant structural role in modulating dopamine D2-like receptor pharmacology.
- The findings expand the known conformational landscape of these receptors.
- This knowledge can inform the design of novel therapeutics targeting dopamine receptors.
Related Concept Videos
01:27Adrenergic Neurons: Neurotransmission
6.0K
Postganglionic sympathetic fibers (except those supplying the sweat glands) releasing noradrenaline or norepinephrine are called noradrenergic or adrenergic neurons. Noradrenaline, dopamine, adrenaline, or epinephrine are collectively called "catecholamines" as they contain a catechol moiety and an amine side chain. The five stages of neurotransmitter release involve their synthesis, storage, release, reuptake and metabolism.
Synthesis: Catecholamine synthesis requires tyrosine, which...
Synthesis: Catecholamine synthesis requires tyrosine, which...
6.0K
01:15Cholinergic Receptors: Nicotinic
6.8K
Nicotinic receptors are ligand-gated ion channels that are activated by acetylcholine and nicotine. Upon activation, they cause a rapid increase in the permeability of cells to K+, Na+, and Ca2+, followed by depolarization and excitation. They are in the autonomic ganglia, skeletal neuromuscular junction, CNS, and adrenal medulla.
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
There are two types of nicotinic receptors: neuromuscular (NM/NM/N1) and neuronal (NN/NN/N2). The two families differ based on their location and selectivity to...
6.8K
01:26Adrenergic Receptors: β Subtype
4.6K
β-adrenoceptors have varied sensitivities towards adrenaline, noradrenaline, and isoprenaline. The order of agonist potency is as follows:
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors...
4.6K
01:29Drugs Affecting Neurotransmitter Synthesis
2.6K
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,...
2.6K
01:22Opioid Receptors: Overview
6.9K
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,...
6.9K
01:26Neurochemical Transmission: Sites of Drug Action
4.0K
Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
4.0K