pharmacodynamics

Question 1

agonist

Answer 1

causes active change of target (excitation or inhibition)

Question 2

antagonist

Answer 2

occupies site and prevents agonist from binding

Question 3

specific binding

Answer 3

binding to receptor

Question 4

non-specific binding

Answer 4

binding to cell membrane

Question 5

competitive binding

Answer 5

binding at active site

Question 6

non-competitive binding

Answer 6

binding at allosteric site

Question 7

benzodiazepines and barbiturates are examples of

Answer 7

allosteric agonists

Question 8

pumps function at what type of enzyme kinetics

Answer 8

saturable (zero order)

Question 9

MDR transporters and Na+/K+ ATPase pumps are an example of what type of transporter

Answer 9

pump

Question 10

lidocaine

Answer 10

voltage-gated Na+ channel blocker

Question 11

dihydropiridine

Answer 11

L-type Ca+2 channel blocker (allosteric modulator)

Question 12

fluoxetine blocks the serotonin selective reuptake, an example of what type of target

Answer 12

symport transporter

Question 13

furosemide block what

Answer 13

Na+/K+/Cl-2 symport transporter

Question 14

digoxin blocks

Answer 14

Na+/Ca+2 exchanger (antiport transporter)

Na+/K+ ATPase

Question 15

CYP2C9 inhibitors

Answer 15

penecillin and azoles

Question 16

CYP2C9 inducers

Answer 16

phenytoin, alcohol, ginseng

Question 17

if you induce enzyme activity, drug level ___

Answer 17

decrease

Question 18

if you inhibit enzyme activity, drug level ___

Answer 18

increases

Question 19

4 types of receptor interactions

Answer 19

1. ion channels
2. GPCR
3. enzyme-linked receptor
4. diffuse through membrane

Question 20

ion channels have how many transmembrane domains

Answer 20

5

Question 21

how many transmembrane domains does a GPCR have

Answer 21

7

Question 22

G proteins have how many subunits

Answer 22

3 (a, b, g)

Question 23

competitive antagonist

Answer 23

binds to active site and blocks agonist from binding, so nothing happens

Question 24

non-competitive antagonist

Answer 24

binds to allosteric site and decreases the effect of the agonist

Question 25

non-competitive agonist

Answer 25

binds to allosteric site and increases the effect of the agonist

Question 26

ligand-gated channels or ROC: # of binding sites

Answer 26

2

Question 27

what is the subunit where the ligand binds on an ROC

Answer 27

alpha

Question 28

ROCs or ligand-gated channels have how many subunits

Answer 28

5

Question 29

nicotinic Ach receptor is a type of

Answer 29

ROC

Question 30

nicotinic Ach receptor: location of ligand-binding site

Answer 30

outside of cell near amino terminal

Question 31

GABA-A receptor is a type of

Answer 31

ROC

Question 32

how many transmembrane proteins does GPCR have

Answer 32

7

Question 33

where is the ligand-recognition site for GPCR

Answer 33

hidden within the cell membrane between 2nd and 3rd domain

Question 34

where is the g protein-coupling domain in GPCR

Answer 34

at the 3rd intracellular loop

Question 35

4 steps for g protein pathway

Answer 35

1. ligand binds to GPCR 2. g protein activates adenylyl cyclase 3. adenylyl cyclase: ATP -> cAMP 4. protein kinase A uses cAMP to phosphorylate

Question 36

steps for g protein activation

Answer 36

1. agonist binds 2. GTP-GDP exchange (g-protein binds to GTP) 3. g protein is activated

Question 37

steps after g protein is activated

Answer 37

1. alpha-GTP binds to effector (adenylyl cyclase) 2. effector is activated 3. agonist unbinds 4. GTP hydrolyzed 5. g protein formed again

Question 38

2 main effector proteins in the GPCR pathway

Answer 38

- adenylyl cyclase | - phospholipase C (PLC)

Question 39

phospholipase C converts what to what

Answer 39

PIP2 -> IP3 + DAG

Question 40

what does IP3 do

Answer 40

stimulates vesicles to release Ca+2

Question 41

what does DAG do

Answer 41

activates PKC

Question 42

what do these G proteins do?: Gi, Gs, G12, Gq

Answer 42

Gi inhibits | Gs, G12, and Gq activate

Question 43

which G proteins activate adenylyl cyclase

Answer 43

Gi and Gs

Question 44

which G proteins activate phospholipase C

Answer 44

G12 and Gq

Question 45

for a proteinase-activated receptor (PAR), cleavage at the amino terminal will cause

Answer 45

activation of the PAR

Question 46

can PARs be activated again?

Answer 46

no, because cleavage cannot be reversed

Question 47

location of ligand-recognition site for enzyme-linked receptor

Answer 47

outside of cell near amino terminal

Question 48

steps when ligand binds to enzyme-linked receptor

Answer 48

1. ligand binds 2. dimerization 3. autophosphorylation 4. Grb2 binds and gets phosphorylated 5. Activation of Ras/Raf/MAP kinase pathway

Question 49

example of enzyme-linked receptors

Answer 49

receptor tyrosine kinase (for growth factors and insulin)

Question 50

cytokine receptors follow the ___ pathway

Answer 50

Jak/Stat

Question 51

what is unique about the Jak/Stat pathway

Answer 51

- no catalytic domains - Stat dimer has 2 NLS - moves into nucleus to bind to genes

Question 52

ANP and Nitric Oxide (NO) receptors are part of what pathway

Answer 52

guanylyl recptor cyclases

Question 53

Class I receptors location

Answer 53

cytoplasm

Question 54

Class II receptors location

Answer 54

nucleus

Question 55

function of chaperones

Answer 55

bound to receptor to prevent accidental translocation to nucleus

Question 56

how are the DNA and ligand binding sites ordered

Answer 56

N-DNA -Ligand - C

Question 57

examples of class 1 receptors

Answer 57

estrogen, progesteron, and androgen receptors, corticosteroid receptors

Question 58

steps of agonist binding to LBD on class 1 receptor

Answer 58

- ligand binds - AF2 binds to LBD - co-activator protein binds to LBD

Question 59

what happens when the antagonist binds to LBD on class 1 receptor

Answer 59

- antagonist prevents AF2 from binding to LBD | - co-activator protein cannot bind also

Question 60

examples of class 2 receptor

Answer 60

- vitamin d3 receptor | - thyroid hormone receptor

Question 61

inflammatory response is mediated by what type of receptors

Answer 61

class 2 receptors