Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

4.3K
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.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
4.3K
Drug-Receptor Interaction: Antagonist01:28

Drug-Receptor Interaction: Antagonist

4.9K
An antagonist is a drug that binds strongly to a receptor without activating it. An antagonist prevents other molecules, such as neurotransmitters or hormones, from binding to the receptor and triggering a cellular response. Such interaction effectively hinders the normal physiological processes mediated by the receptor, resulting in various pharmacological effects depending on the specific receptor targeted.
Antagonists can be classified as competitive or noncompetitive based on their...
4.9K
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

3.9K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
3.9K
Adrenergic Agonists: Direct-Acting Agents01:30

Adrenergic Agonists: Direct-Acting Agents

2.7K
Drugs that mimic the action of endogenous catecholamines like noradrenaline and adrenaline are called adrenergic agonists or sympathomimetics. Based on their mechanism of action, sympathomimetics can be classified as direct-, indirect-, or mixed-acting sympathomimetics. Direct-acting adrenergic agonists activate adrenoceptors without affecting presynaptic neurons, making them independent of neuronal catecholamine-depleting agents like reserpine and guanethidine.
These agents can be classified...
2.7K
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:29

Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

1.1K
Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
1.1K
Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers01:17

Adrenergic Antagonists: Chemistry and Classification of ɑ-Receptor Blockers

1.7K
Adrenergic antagonists, or sympatholytics, inhibit adrenoceptor activation driven by catecholamines or agonists. Based on their adrenoceptor specificity, adrenergic blockers can be categorized into two primary groups: α-adrenergic blockers (α-blockers) and β-adrenergic blockers (β-blockers). α-blockers interact with α1 and α2 subtypes of α-adrenoceptors.
Nonselective α-blockers: Nonselective α-blockers contain haloalkylamine or imidazoline...
1.7K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

Sweet and umami TAS1R receptors: from molecular recognition to physiological function.

Chemical senses·2026
Same author

Glutathione as a taste modulator: molecular mechanisms of interaction with umami and sweet taste receptors.

Food chemistry. Molecular sciences·2025
Same author

Distinct odorant receptor response patterns to aliphatic odorants in freely behaving mice.

Chemical senses·2025
Same author

How allosteric mutations control ligand binding in Lipocalin protein: odorant binding protein as a test case.

Cellular and molecular life sciences : CMLS·2025
Same author

Accelerating Ligand Discovery for Insect Odorant Receptors.

International journal of biological sciences·2025
Same author

Ligand discrimination in hOR1A1 based on the capacitive response.

Biosensors & bioelectronics·2024

Related Experiment Video

Updated: Apr 26, 2026

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase
09:53

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase

Published on: April 23, 2019

6.5K

Discrimination between olfactory receptor agonists and non-agonists.

Jérémie Topin1, Claire A de March, Landry Charlier

  • 1Université de Nice - Sophia Antipolis, Institut de Chimie de Nice UMR 7272, Parc Valrose 28, Avenue Valrose 06108, Nice, Cedex 2 (France).

Chemistry (Weinheim an Der Bergstrasse, Germany)
|July 22, 2014
PubMed
Summary

Researchers combined computational simulations and lab experiments to understand how a human olfactory receptor (1G1) binds to odorants. This approach successfully identified which molecules activate the receptor, proving useful for discovering new receptor-ligand interactions.

Keywords:
calcium imagingfree energymolecular modelingodorantsreceptors

More Related Videos

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay
09:11

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay

Published on: October 2, 2017

8.7K
High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity
12:02

High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity

Published on: June 2, 2014

11.6K

Related Experiment Videos

Last Updated: Apr 26, 2026

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase
09:53

Real-time In Vitro Monitoring of Odorant Receptor Activation by an Odorant in the Vapor Phase

Published on: April 23, 2019

6.5K
Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay
09:11

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay

Published on: October 2, 2017

8.7K
High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity
12:02

High-throughput Analysis of Mammalian Olfactory Receptors: Measurement of Receptor Activation via Luciferase Activity

Published on: June 2, 2014

11.6K

Area of Science:

  • Computational chemistry
  • Molecular dynamics simulations
  • Olfactory receptor research

Background:

  • Olfactory receptors (ORs) are crucial for smell perception.
  • Understanding ligand-receptor interactions is key to deorphanizing ORs.
  • The human 1G1 OR is broadly tuned, making its ligand specificity challenging to determine.

Purpose of the Study:

  • To computationally deorphanize the human 1G1 olfactory receptor.
  • To validate a combined computational and experimental approach for predicting odorant binding.
  • To demonstrate the utility of free-energy calculations in olfactory receptor research.

Main Methods:

  • Free-energy calculations using molecular-dynamics simulations.
  • Calcium-imaging assays to experimentally determine agonist activity.
  • Joint analysis of computational and experimental data for ten odorants.

Main Results:

  • Successfully computed the free energy of binding for ten odorants to the 1G1 receptor.
  • Differentiated between eight experimentally determined agonists and two non-agonists.
  • Validated the predictive power of free-energy calculations for OR deorphanization.

Conclusions:

  • The combined computational and experimental approach is a powerful tool for OR deorphanization.
  • Free-energy calculations can accurately predict odorant binding and activity.
  • This study provides a proof-of-principle for computational deorphanization of olfactory receptors.