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

Principles of Drug Action01:24

Principles of Drug Action

Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Pharmacodynamics: Overview and Principles01:21

Pharmacodynamics: Overview and Principles

Pharmacodynamics is a scientific field that delves into drugs' intricate biochemical, cellular, and physiological effects on the human body. The study of pharmacodynamics helps us understand how drugs interact with the body and elicit various responses.
Most drugs' effects result from their interactions with drug receptors or targets within the body. These interactions trigger specific responses at the cellular or systemic level. Drug receptors can be found on the surfaces of cells or within...
Drug-Receptor Interactions01:29

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

You might also read

Related Articles

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

Sort by
Same author

Reining in Unbridled AI Enthusiasm: Protecting the Integrity of Rehabilitation Science and Clinical Care.

Archives of physical medicine and rehabilitation·2026
Same author

Through their eyes': A qualitative study on the impact of virtual reality on parents' understanding of visual impairment.

Eye (London, England)·2026
Same author

Biased Signaling as Allosteric Probe Dependence: Everything Old Is New Again.

Biochemistry·2026
Same author

Therapeutic implications of target residence time.

Current opinion in structural biology·2026
Same author

Evaluating the Use of Google Street View to Visually Verify the Locations of Cannabis Retailers in the United States Extracted from Websites, 2015-2018.

Applied spatial analysis and policy·2026
Same author

Kinetics of De Novo Bone and Bone Marrow Niche Formation With Hybrid Click Cryogels.

Advanced healthcare materials·2026
Same journal

Methylated SNHG3 lncRNA counteracts PSMD4-inhibited angiogenesis by HnRNPA2B1 SUMOylation in peripheral arterial disease.

Biochemical pharmacology·2026
Same journal

The organelle-targeting duality of nanomaterials: physicochemical property-guided therapeutic effects and toxicological outcomes.

Biochemical pharmacology·2026
Same journal

The central role of endoplasmic reticulum stress in Parkinson's disease and targeted therapeutic strategies.

Biochemical pharmacology·2026
Same journal

Mechanisms involved in the regulation of carbohydrate and lipid metabolism by oleanane-type pentacyclic triterpenes.

Biochemical pharmacology·2026
Same journal

Myricitrin alleviates paraquat-induced acute lung injury via PERK pathway to attenuate endoplasmic reticulum stress and mitochondrial dysfunction.

Biochemical pharmacology·2026
Same journal

Design, synthesis, and biological evaluation of Combretastatin A4 dimers for the treatment of hepatocellular carcinoma.

Biochemical pharmacology·2026
See all related articles

Related Experiment Video

Updated: May 8, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
05:10

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

Defining and characterizing drug/compound function.

Terry Kenakin1, Michael Williams2

  • 1Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, United States.

Biochemical Pharmacology
|August 20, 2013
PubMed
Summary
This summary is machine-generated.

Receptor theory, foundational to understanding disease and drug action, has evolved with molecular biology. Modern concepts like biased signaling enhance drug discovery by detailing complex compound-target interactions.

Keywords:
Compound functionReceptor theoryReceptors

More Related Videos

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

Related Experiment Videos

Last Updated: May 8, 2026

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System
05:10

Drug Repurposing Hypothesis Generation Using the "RE:fine Drugs" System

Published on: December 11, 2016

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Drug Discovery

Background:

  • The receptor concept is central to understanding disease mechanisms and drug actions.
  • Receptor theory, established over a century ago, has advanced significantly with molecular biology tools.

Purpose of the Study:

  • To explore the evolution of the receptor concept in pharmacology.
  • To highlight how advanced research technologies have refined the understanding of drug/ligand-receptor interactions.
  • To discuss the integration of new concepts into drug discovery.

Main Methods:

  • Review of historical and modern receptor theory.
  • Analysis of molecular biology and research technology advancements.
  • Examination of concepts such as allosterism, inverse agonism, and biased signaling.

Main Results:

  • Receptor theory has evolved, incorporating complex molecular-level interactions.
  • New concepts provide a more nuanced understanding of drug action beyond simple agonism/antagonism.
  • Pharmacological data can now predict drug effects across different systems.

Conclusions:

  • The modern receptor concept, enriched by molecular insights, offers a sophisticated framework for drug discovery.
  • Understanding pleotropic effects and signaling pathways is crucial for predicting drug efficacy.
  • Advanced receptor pharmacology informs the development of targeted therapeutics.