Course Prerequisites

Students must have completed course work in biology and chemistry before taking this course.

This course does require the student to have access to a computer, and a proficiency in the use of microcomputers.

Course Content

This course will consist of eight lessons and three workshops.

Each lesson will include specific readings. Students will also be required to participate in a discussion forum during the course.

Course Objectives

The object of this part of the course is to provide the foundation necessary for understanding receptor-ligand (receptor-drug) interactions, and the fundamentals of the techniques commonly employed for such analysis. It is expected that at the end of this section, all students will be able to design and/or interpret studies that characterize either new receptors, or new drugs.

Course Materials
 

	TextbooksThe following texts will be most useful for students in this class LE Limbird. Cell surface receptors: A Short Course on Theory and Methods, Second Edition. Kluwer Academic Publishers, 1996.  HI Yamamura et al. Methods in Neurotransmitter Receptor Analysis, Raven Press, 1990. T Kenakin. Pharmacologic Analysis of Drug Receptor Interaction (2nd ed.) Raven Press, 1993.
	Internet materials E-mail -- Students may communicate with me at any time during the course via e-mail.

Course Outline

Session 1: Receptor terminology, law of mass action
Brief Historical Background
• Some terms and definitions
• The pharmacologist?s dream
Theories of Drug-Receptor Interaction
• Law of mass action
• The theoretical basis for characterizing receptors using saturation radioligand assays
Session 2: Introduction to theory, practice of radioligand binding
Radioactivity, radioligands and binding assays
• How to separate Bound from Free
• Total vs. free concentrations of ligand. Ligand Depletion
• Radioactivity
• Selecting the Radioligand
Session 3: Receptor/radioligand characterization: saturation isotherms, kinetic analysis
Characterization of a Receptor Using a Radioligand
• Analysis of saturation radioligand binding data
Workshop 1: Radioactivity and saturation experiments
 
Session 4: Competitive binding I: one class of receptors
Determination of Kinetic Parameters
• Dissociation binding data
• Association binding data
Session 5: Competitive binding II: multiple receptors and complex data
Competitive Binding Data with One Clase of Receptors
• Shallow competitive Binding Curves
• Ligand, Prism and Other Curve Fitting Programs
Session 6: Schild analysis and principles of antagonism
Antagonism
• Competitive Antagonism
• Schild Regression
• Noncompetitive Antagonism
Workshop 2: Characterization of drugs and receptors via competitive analysis and mechanisms of antagonism

Session 7: Partial Agonists

Partial Agonists
• What does a partial agonist look like?
• Estimating the potency of partial agonists
• Decreasing receptor concentration
Session 8: Characterization of new cloned receptors and drug design strategies

Workshop/discussion 3: (partial agonists or new receptors and drugs??)

Grading Information

One of the ways we will assess progress will be with short (10 min maximum) quizzes that we give at the beginning of many (but not all classes). These quizzes will be an important part of your grade. We shall throw out your two lowest grades so that if you miss a quiz or do poorly on one or two, it will not adversely impact your grade. Because we can proceed in more depth if the assigned reading has been done, the quizzes may cover some of this material. Your assignments for the next class will be clearly delineated.

Assigned problem sets and class participation will also be important components of grading (especially because it helps us gauge progress).

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Dr. Mailman can be reached via email at rmailman@css.unc.edu


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Page created by Nancy Underwood, 7/31/97
Page content by Richard Mailman, Ph.D. 7/31/97

Copyright 1997 by Richard Mailman and Jose Boyer. All rights reserved.