Full agonists produce a maximal response. Partial agonists cannot and are less effective.
Potentiation of an agonist shifts the dose-response curve to L or R?
Left
Antagonism of an agonist shifts the dose-response curve to L or R?
Right
What is the ED50?
The dose of a drug that is effective in 50% of the patient population
A steep slope for a cumulative dose response curve means what?
There is little variability in drug response in a given population. The less steep the slope, the greater the variability in patient sensitivity to the effects of a drug.
What is the TD50?
The dose that is toxic to 50% of the patient population.
What is the LD50?
The dose that is lethal to 50% of the patient population.
What is the therapeutic index?
Evaluates the relative safety of a drug.
A drug with a lower therapeutic index means what?
That the doctor needs to be more careful in the dosing of the drug for a patient because there is only a small therapeutic window in terms of the dosing.
What happens when an agonist binds to a Gs receptor?
activation of adenylyl cyclase --> increase in cAMP
Mnemonic to remember the G-protein-coupled ANS receptors.
Kiss and kick til you're sick of sex. qiss qiq siq sqs = a1 a1 B1 B2, M1 M2 M3, D1 D2 H1, H2 V1 V2
What happens when Gi receptors are stimulated?
inhibition of adenylyl cyclase --> decrease in cAMP
What happens when Gq receptors are stimulated?
activation of phospholipase C
What happens when endothelial cells release NO?
NO --> activation of guanylyl cyclase --> increases cGMP in smooth muscle --> myosin light chains are dephosphorylated --> myosin can't interact with actin --> vasodilation