Standard Article

Receptor Identification and Characterization

Handbook of Physiology, The Endocrine System, Cellular Endocrinology

  1. Lee E. Limbird1,
  2. Harvey Motulsky2

Published Online: 1 JAN 2011

DOI: 10.1002/cphy.cp070104

Comprehensive Physiology

Comprehensive Physiology

How to Cite

Limbird, L. E. and Motulsky, H. 2011. Receptor Identification and Characterization. Comprehensive Physiology. 49–67.

Author Information

  1. 1

    Vanderbilt University Medical Center, Department of Pharmacology, Nashville, Tennessee

  2. 2

    GraphPad Software, Inc., San Diego, California

Publication History

  1. Published Online: 1 JAN 2011

Abstract

The sections in this article are:

  • 1
    Identification of Receptors Based on Functional Properties
    • 1.1
      Schild Analysis
  • 2
    Identification of Receptors with Radioligand Binding
    • 2.1
      Choosing the Biological Preparation
    • 2.2
      Choosing a Radioligand
    • 2.3
      Separating Bound From Free Radioligand
    • 2.4
      Irrelevant Binding
    • 2.5
      Establishing That the Radioligand Binding Detected Reflects Interaction With the Physiologically Significant Receptor
    • 2.6
      Analysis of Radioligand Binding Data Based on the Law of Mass Action
    • 2.7
      Fractional Occupancy
    • 2.8
      Assumptions Inherent in the Law of Mass Action
  • 3
    Saturation Binding Studies
    • 3.1
      Defining Nonspecific Binding in a Radioligand Binding Assay
  • 4
    Defining The Specificity of Radioligand Binding Using Competitive Binding Analysis
    • 4.1
      Analyzing Competitive Binding Data
    • 4.2
      Calculating the Ki From the IC50
    • 4.3
      Homologous Competitive Binding Curves Permit an Assessment of Both Kd and Bmax
  • 5
    Kinetic Analysis of Radioligand Binding Experiments
    • 5.1
      Studies of Radioligand Dissociation
    • 5.2
      Studies of Radioligand Association
  • 6
    Complex Binding Phenomena
    • 6.1
      Competitive Binding Experiments With Two (or More) Receptor Sites
    • 6.2
      Saturation Binding Experiments With Two Receptor Sites
    • 6.3
      Comparing One- and Two-Site Models
    • 6.4
      The Slope Factor of a Competitive Binding Curve
    • 6.5
      Using Dissociation Experiments to Investigate Complex Binding
    • 6.6
      Distinguishing Between Independent Receptor Subtypes and Negative Cooperativity
    • 6.7
      Evaluating Allosteric Phenomena
    • 6.8
      Obtaining Independent Data to Clarify the Biological Origin of Complex Binding Phenomena
    • 6.9
      Agonist Binding and the Ternary Complex
  • 7
    Summary