**pharm Test 1 - Lecture 3 - Receptors

Front 1

What are the 4 types of drug receptors?

Back 1

Ligand gated ion channel (IONOTROPIC
G-protein coupled (METABOTROPIC)
Kinase-linked receptors
Nuclear receptors

Front 2

Define ED50

Back 2

1/2 maximal response

Front 3

define Emax

Back 3

maximal response

Front 4

Define EC50

Back 4

the conc of an agonist giving 50% of the maximal response

Front 5

describe drug-receptor interactions effect on equilibrium

Back 5

e. The drug-receptor interaction can either move equilibrium towards and increase or decrease in affinity. Agonists will favor the binding of a drug to a receptor and antagonist will reduce the affinity.
f. At equilibrium, receptor occupancy is related to drug concentration. The higher the affinity of the drug for the receptor, the lower the concentration at which it produces a given level of occupancy, but not necessarily greater effect.
g. In the resting state (when there is not a ligand bound to the receptor) the equilibrium normally favors the resting state.
h. When a full agonist binds preferentially to the activated state, it shifts the equilibrium towards activation. An agonist initiates changes in cell function. Full agonists produce maximal effects, while partial agonists produce only submaximal effects.
i. A partial agonist shows less selectivity and shifts the equilibrium to a smaller extent, even when receptors are fully occupied.
j. An antagonist shows no preference and does not shift the equilibrium, though it reduces the effect of an agonist by preventing the agonist from binding to the receptors. An antagonist binds to receptors without initiating changes in cell function

Front 6

Signaling molecule actually doesn't ___A___, uses cascade of events to ___B___ cellular change. Use receptors on ___C___ which are usually coupled to ___D___ on the __E___surface of the membrane. (D) then __F__es another molecule, usually ___G___ which carries further action.

Back 6

A- enter the cell
B - induce
C- plasma membrane
D - kinase
e -inner
F - phosphorylates
G - cAMP

Front 7

from an LDR curve, what is the X axis? what is the Y-axis?
Where do you gain info of the efficacy? the potency?

Back 7

x = dose of drug
Y = % maximal response
x = potency
y = efficacy

Front 8

if an LDR curve shows 2 parallel lines, the 2 drugs have similar____

Back 8

mechanism of action

Front 9

what does this LDR curve illustrate?

Back 9

reversible competitive inhibition

Front 10

what does this LDR curve illustrate?

Back 10

irreversible competitive inhibition

Front 11

what does this LDR curve illustrate?

Back 11

allosterism w/ potentiation

Front 12

what does this LDR curve illustrate?

Back 12

non-competitive allosterism w/ antagonism

Front 13

A ____antagonist has the opposite physical effect of a drug

Back 13

physiological

Front 14

a____antagonist effcts the absorption/metabolism of another drug

Back 14

pharmacokinetic