The lesson centered around the question; What happens when a drug and a endogenous ligand have affinity for the same receptor?
Discuss the relative concentrations of drug and ligand. Discuss the structural and chemical similarities.
Examine non receptor antagonists, antibodies, neutralization chemicals and physiological barriers.
Use examples like tamoxifen to block estrogen in breast cancer, and naloxone to block morphine agonists.

Distinguish between agonist and antagonist ligands.
Discuss active, inactive and inactivated receptors-
Indicate agonists can be full, partial, or inverse.
Discuss how antagonists inhibit the activation of an agonist
Indicate potency, efficacy, and safety as the main criteria
Discuss the relationship between concentration and response.
Indicate graded dose response and quantal dose response.

Explain the two conformational states of receptors, active and inactive.
Indicate how binding to one or the other will determine the function (action) of the drug.
The actions will either be agonist or antagonist actions
Agonists are ligands which will enhance the natural reaction of the body.
Relate potency to affinity to the receptor as a direct relationship
Introduce antagonist ligands.

Describe quantal relationship as the concentration of drug that will produce a given effect in a population.
Explain how the effect is seen over aa range of doses, and that the response is either present or not present: sleep or no sleep, alive or not alive.
Using graphs, discuss the three types of responses seen.
Effectiveness ( ED50), toxicity (TD50) and lethal effect(LD50)

Read and discuss an article from the Merck Manual which reviews and defines the drug-receptor complex which we have been covering. This article was a professional review article.
It contained all the terminology and binding sciece we have been discussing.

Discuss the quantification of dose-response of a drug based on the number of occupied receptors.
Show using graphs how the response to a drug is proportional to the concentration of occupied receptors.
Define both graded and quantal relationships.
Discuss potency and efficacy by viewing the EC50 and the E max on a graph.

Discuss drug tolerance as a function of more receptors being synthesized in order to achieve the same response.
View an analyze a linear dose response curve and compare it to a log dose response curve.
Show how the % of maximal response can be more accurately determined using the log curve at very low doses.

Use graphs and diagrams to show the effect of the concentration of ligand-receptors on a drug response.
Discuss rational drug design, intended to lower adverse affects and increase potency

Lesson is the one outlined for Monday

Discuss how the structure of a drug affects its ability to gain access to a receptor.
Water soluble drugs versus fat soluble drugs
Examine how rational drug design can allow for optimal binding to receptors, reduction in toxicity, and increase in efficiency