Lecture set 2

Question 1

Agonist vs antagonist

Answer 1

Both bind to the same receptor site and induce a conformational change but an agonist will enhance activation of the receptor where as antagonist will block activation and also block any agonist or ligands from binding to the receptor

Question 2

identify and compare dose response curves for each type of ligand in the ligand spectrum

Answer 2

Full Inverse Agonist: full opposite activity
Partial Inverse Agonist: slight opposite activity
Silent Antagonist: no activity
Partial Agonist: less enhanced activity
Full Agonist: full enhanced activity
Super Agonist: causes a response that is greater than the endogenous ligand

Question 3

use graphical data to compare potency and efficacy for active ligands

Answer 3

potency is a dose of a drug required to produce a particular effect
efficacy is the biological response resulting from the drug receptor interaction

Question 4

describe the concept of a partial agonist

Answer 4

Produces a reduced response event at full receptor occupancy
It decreases the maximal response even if we increase the concentration of partial antagonist

Question 5

apply the concept of partial agonist theory to managing drug therapy

Answer 5

?

Question 6

describe the features of an inverse agonist

Answer 6

needs the receptor to spontaneously activate so it doesn’t need a drug to activate
it can be full or partial
bind to the orthosteric side so the response of the agonist can be modulated by other agonist and antagonist

Question 7

compare reversible competitive and irreversible noncompetitive inhibition

Answer 7

They both bind to the orthosteric site of the receptor and at first the curves will look the same as they shift the curve to the right thus increasing EC50. overtime the noncompetitive will begin to decrease the Emax. Competitive will not to do this because we can outcompete the inhibitor if we increase concentration of the drug thus producing the Bmax

Question 8

use the concept of spare receptor to explain drug action

Answer 8

Maximal response can be elicited by agonist at a concentration that does not result

Question 9

describe chemical and functional antagonism

Answer 9

Chemical antagonism - chemical reaction occurs between an agonist and an antagonist to form an inactive product
Functional antagonist- two drugs influence a physiological system but in opposite directions

Question 10

describe the mechanism of allosteric modulators and their potential benefit in drug therapy

Answer 10

bind at sites unique from the agonist
with allosteric modulators we can increase or decrease both potency and efficacy of a drug to improve the therapy use