General Features of Receptors
Agonist Def.
Antagonist Definition
2 Critical Features of Receptors
For almost all drugs the dose response curve is….
Dose Response Curve for Almost All Drugs
How does a dose response curve look when it’s in a semilog plot
Plotting Equation for Linear or Semilog
Def. of Potency
Def. of Efficacy
Relationship between Potency and Efficacy
Alt Eqn for semilog or linear plot
Values of Range of Binding/Response
100 Fold
Dose Response Curve for 4 different Analgasic Drugs
Explain the Potency and Efficacy of these 4 Drugs
Explain this Graph
Cool Quote by Paracelsus
Explain the Concept of Quantal Response
Def and Eq. of Therapuetic Index
Margin of Safety
Doses that cause side effects…
Plot of Therapuetic Index vs. MoS
Aspirin: Therapuetic Effect, Side Effect, Lethality
Effect vs. Agonist
Binding Vs. Agonist
Spare Receptors
Advantages of Spare Receptors
Spare Receptors and Proof of Less Desensitizaiton
Spare Receptors and Greater Sensitivity
Spare Receptors, Increased Sensitivity, and Drug Concentration
Drug Binding and Dissociation Constant
Lower Kd and Range
Variability of on rates vs. off rates
Kd and Implications of choosing a drug
Efficacy and Potency for Partial and
Efficacy of Partial Agonist vs. Full Agonist
Proper dose of Partial agonist and baseline
Lowering the Full Agonist Response
Partial agonist intervention compared to full agonists or antagonists
Buprenorphine
Buprenorphine Response Curve
Agonists, antagonists, and efficacy
Can we account for full agonists, partial agonists, and antagonists with one simple model?
R to R model
R to R model of Action for agonists, partial agonists, antagonists, and reverse agonists
Inverse Agonist
Summary of Agonists, Partial Agonists, Antagonists, and Inverse Agonists