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

The Two-State Receptor Model01:29

The Two-State Receptor Model

The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with one...
Introduction to Sensory Receptors01:31

Introduction to Sensory Receptors

Sensory receptors are vital in our ability to perceive and interpret the world. Sensory receptors are specialized cells in the peripheral nervous system that respond to various stimuli and enable one to experience different sensations. Based on specific criteria, sensory receptors are classified into distinct types.
The first classification criterion is based on cell type, position, and function. Some receptor cells are neurons with free nerve endings, where their dendrites are embedded in the...
Types of Receptors: Cell Surface Receptors01:28

Types of Receptors: Cell Surface Receptors

Cell-surface receptors, also known as transmembrane receptors, are cell surface, membrane-anchored (integral) proteins that bind to external ligand molecules. This type of receptor spans the plasma membrane and performs signal transduction, converting an extracellular signal into an intracellular signal. Ligands that interact with cell-surface receptors do not have to enter the cell that they affect. Cell-surface receptors are also called cell-specific proteins or markers because they are...
Internal Receptors01:31

Internal Receptors

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.
Internal Receptors01:31

Internal Receptors

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.
Introduction to Special Senses01:26

Introduction to Special Senses

Sensory receptors play an integral part in comprehending our external and internal environments. They receive diverse stimuli, converting them into the nervous system's electrochemical signals. This conversion occurs as the stimulus alters the sensory neuron's cell membrane potential, instigating the generation of an action potential. This action potential is subsequently transmitted to the central nervous system (CNS), which integrates with other sensory data or higher cognitive functions.

You might also read

Related Articles

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

Sort by
Same author

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

BiochemistryĀ·2026
Same author

Therapeutic implications of target residence time.

Current opinion in structural biologyĀ·2026
Same author

Structure-based design of an opioid receptor modulator for enhanced morphine analgesia.

Science advancesĀ·2026
Same author

Differential Effects of Sodium on Agonist-Induced Conformational Transitions and Signaling at Ī¼ and Īŗ Opioid Receptors.

BiochemistryĀ·2025
Same author

Agonism and Biased Signaling.

Handbook of experimental pharmacologyĀ·2025
Same author

Differential effects of sodium on agonist-induced conformational transitions and signaling at Ī¼ and Īŗ opioid receptors.

bioRxiv : the preprint server for biologyĀ·2025
Same journal

Targeted Protein Degradation Phenotypic Studies Using HaloTag CRISPR/Cas9 Endogenous Tagging Coupled with HaloPROTAC3.

Current protocols in pharmacologyĀ·2020
Same journal

Preclinical Models for Studying the Impact of Macrophages on Cancer Cachexia.

Current protocols in pharmacologyĀ·2020
Same journal

In Vitro Permeation Test (IVPT) for Pharmacokinetic Assessment of Topical Dermatological Formulations.

Current protocols in pharmacologyĀ·2020
Same journal

A Localized Aldara (5% Imiquimod)-Induced Psoriasiform Dermatitis Model in Mice Using Finn Chambers.

Current protocols in pharmacologyĀ·2020
Same journal

Autologously Humanized Mice for Immune-Oncologic Studies.

Current protocols in pharmacologyĀ·2020
Same journal

Establishment of Humanized Mice from Peripheral Blood Mononuclear Cells or Cord Blood CD34+ Hematopoietic Stem Cells for Immune-Oncology Studies Evaluating New Therapeutic Agents.

Current protocols in pharmacologyĀ·2020
See all related articles

Related Experiment Video

Updated: May 25, 2026

A BW Reporter System for Studying Receptor-Ligand Interactions
06:05

A BW Reporter System for Studying Receptor-Ligand Interactions

Published on: January 7, 2019

Receptor theory.

Terry Kenakin1

  • 1GlaxoSmithKline Research Institute, Research Triangle Park, North Carolina, USA.

Current Protocols in Pharmacology
|February 2, 2012
PubMed
Summary
This summary is machine-generated.

Receptor theory uses mathematical models to quantify drug effects and predict biological system responses. This study reviews classical and operational models, exploring drug-receptor interaction mechanisms.

More Related Videos

High-resolution Spatiotemporal Analysis of Receptor Dynamics by Single-molecule Fluorescence Microscopy
15:13

High-resolution Spatiotemporal Analysis of Receptor Dynamics by Single-molecule Fluorescence Microscopy

Published on: July 25, 2014

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Related Experiment Videos

Last Updated: May 25, 2026

A BW Reporter System for Studying Receptor-Ligand Interactions
06:05

A BW Reporter System for Studying Receptor-Ligand Interactions

Published on: January 7, 2019

High-resolution Spatiotemporal Analysis of Receptor Dynamics by Single-molecule Fluorescence Microscopy
15:13

High-resolution Spatiotemporal Analysis of Receptor Dynamics by Single-molecule Fluorescence Microscopy

Published on: July 25, 2014

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

Area of Science:

  • Pharmacology
  • Biomathematics
  • Systems Biology

Background:

  • Drug receptor theory provides quantitative methods to understand drug effects.
  • System-independent drug activity quantification is crucial for therapeutic relevance.
  • Predicting drug effects across diverse biological conditions is essential.

Purpose of the Study:

  • To provide a historical overview of classical receptor theory.
  • To describe the currently used operational model of drug effects.
  • To explain drug-receptor interaction mechanisms.

Main Methods:

  • Review of classical receptor theory.
  • Description of the operational model of drug effects.
  • Explanation of ternary complex, two-state, and probabilistic models.

Main Results:

  • Classical receptor theory offers foundational mathematical rules for biological systems.
  • Operational models provide tools for system-independent drug activity quantification.
  • Ternary complex, two-state, and probabilistic models elucidate drug-receptor interaction mechanisms.

Conclusions:

  • Receptor theory is vital for quantifying drug effects and predicting biological responses.
  • Understanding various receptor models enhances the prediction of drug actions in different physiological states.
  • This review synthesizes historical and current models for a comprehensive view of drug receptor function.