Related Experiment Video
Updated: Nov 28, 2025
08:49
Rapid In Situ Hybridization using Oligonucleotide Probes on Paraformaldehyde-prefixed Brain of Rats with Serotonin Syndrome
Published on: September 23, 2015
9.1K
Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.
Eric Gibbs1, Sudha Chakrapani2,3
1Department of Physiology and Biophysics, Case Western Reserve University, Cleveland, OH, 44106-4970, USA. edg42@case.edu.
Sub-Cellular Biochemistry
|November 30, 2020
Summary
The 5-hydroxytryptamine receptor subtype 3 (5-HT3R) is crucial for gut-CNS signaling and neuronal communication. Recent structural insights illuminate its function, ion permeation, and ligand binding, revealing future research avenues.
Area of Science:
- Neuroscience
- Molecular Biology
- Structural Biology
Background:
- The 5-hydroxytryptamine receptor subtype 3 (5-HT3R) is a pentameric ligand-gated ion channel (pLGIC).
- It plays a key role in gut-central nervous system (CNS) signaling and modulates non-serotonergic synaptic activity.
- Advances in structural biology offer new mechanistic insights into 5-HT3R function.
Purpose of the Study:
- To provide a comprehensive overview of 5-HT3R.
- To detail the mechanisms of ion permeation, ligand binding, and allosteric coupling.
- To highlight progress, challenges, and future opportunities in 5-HT3R research.
Main Methods:
- Literature review and synthesis of biochemical evidence.
- Analysis of structural biology data.
- Physiological context integration.
Main Results:
- Structural advances provide mechanistic understanding of 5-HT3R.
- Detailed insights into ion permeation and ligand binding mechanisms.
- Allosteric coupling between ligand binding and ion channel function is elucidated.
Conclusions:
- Significant progress has been made in understanding 5-HT3R structure and function.
- Outstanding challenges remain in fully elucidating its physiological roles.
- Future research opportunities lie in leveraging structural and biochemical data for therapeutic development.
Related Concept Videos
01:30Transducer Mechanism: G Protein–Coupled Receptors
3.4K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
GPCRs are also called heptahelical,...
3.4K
01:21G-protein Coupled Receptors
129.3K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
129.3K
01:31Adrenergic Receptors: ɑ Subtype
2.5K
Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
2.5K
01:15G Protein-coupled Receptors
15.3K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
15.3K
01:25Cholinergic Receptors: Muscarinic
4.2K
The pharmacological actions of acetylcholine are elicited via its binding to two families of cholinergic receptors or cholinoceptors, namely, muscarinic and nicotinic receptors. Muscarinic receptors are G protein-coupled receptors and have five subtypes, M1–M5. All mAChR subtypes are activated by acetylcholine and blocked by the antagonist, atropine.
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
The subtypes M1, M3, and M5 couple with the Gq subunit and activate the phospholipase C (PLC) activity, mobilizing intracellular Ca2+....
4.2K
01:26Adrenergic Receptors: β Subtype
3.1K
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...
3.1K