Pharmacology Exam 1

Front 1

Which of the following displays the first pass effect

A. liver
B. Small intestine (intraperitoneal route)
C. Large intestine (rectal route)
D. All of the above

Back 1

D. All of the above

(rectal route is minimal due to bypassing of liver)

Front 2

Rank the order of a drug's effect in regards to SPEED:

- Oral
- Intramuscular (IM)
- Subcutaneous (SC)
- Intravenous (IV)

Back 2

IV > IM > SC > Oral

Front 3

Rank the order of a drug's effect in regards to DURATION:

- Oral
- Intramuscular (IM)
- Subcutaneous (SC)
- Intravenous (IV)

Back 3

Oral > SC > IM > IV

Front 4

Which is the most common mechanism of drug transport?

A. active transport
B. Facilitated diffusion
C. pinocytosis / phagocytosis
D. Passive diffusion

Back 4

D. Passive diffusion

Front 5

Drugs always pass between cells because of the presence of gap junctions.

A. both statements are true
B. both statements are false
C. the 1st statement is true, the 2nd statement is false
D. the 1st statement is false, the 2nd statement is true

Back 5

B. both statements are false

- pass THROUGH cells
- TIGHT junctions (zonula occludens)

Front 6

T/F
Larger surface areas absorb drugs FASTER than smaller surface areas.

Back 6

True

Front 7

Food in the stomach will slow down gastric emptying time, which increases the bioavailability of the drug.

A. both statements are true
B. both statements are false
C. the 1st statement is true, the 2nd statement is false
D. the 1st statement is false, the 2nd statement is true

Back 7

C. the 1st statement is true, the 2nd statement is false

(SLOWS ABSORPTION of drug)

Front 8

Many drugs slow gastric emptying and may slow absorption of a ANOTHER drug.

A. both statements are true
B. both statements are false
C. the 1st statement is true, the 2nd statement is false
D. the 1st statement is false, the 2nd statement is true

Back 8

A. both statements are true

Front 9

Which way(s) can a drug pass through a membrane to be absorbed?

A. weak acid in the intestine (basic)
B. weak base in the intestine (basic)
C. weak base in the stomach (acidic)
D. weak acid in the stomach (acidic)

Back 9

B. weak base in the intestine (basic)

D. weak acid in the stomach (acidic)

Front 10

A weakly basic drug is given to a patient intravenously. It takes longer for the drug to be absorbed than a weakly acidic drug. Why?

Back 10

Weak base can still cross the capillaries and gastric mucosa to enter the stomach where they get ionized & trapped.

It get absorbed later when it enters the intestines.

Front 11

An acidic drug with a pKa of 4 enters the stomach (pH 2). Do you expect most of the drug to be well absorbed?

Back 11

Yes

(for an acid, pKa > pH = absorbed)

Front 12

A basic drug with a pKa of 5 enters the stomach (pH 2). Do you expect most of the drug to be well absorbed?

Back 12

No

(for a base, pKa > pH = poorly absorbed)

Front 13

A drug with a pKa of 8 enters the body with a Kp (partition coefficient) of 0.001. Do you expect this to have better absorption than if the Kp was 0.1?

Back 13

No

(smaller Kp = less absorption)
(Kp = Coil / Cwater)

Front 14

What are some factors that can affect the bioavailability?

A. Size of drug
B. type of capsule of pill
C. type of inert ingredients
D. Crystalline properties
E. All of the above

Back 14

E. All of the above

Front 15

Drug measurement in the body is based on _____

A. Intracellular fluid
B. Intravascular fluid (plasma)
C. Interstitial fluid
E. Total body water

Back 15

B. Intravascular fluid (plasma)

Front 16

What is the formula for Volume of Distribution?

Back 16

Vd = dose / Cp

Front 17

What is the formula for Fractional Volume of Distribution?

Back 17

Fract. Vd = Vd / body weight

Front 18

Describe how the following factors INCREASE the RATE of drug distribution:

- Lipid solubility (Kp)
- Ionization (charge)
- Molecular weight
- Blood flow

Back 18

- ↑ Lipid solubility (Kp)
- Electrically neutral
- Low molecular weight
- ↑ Blood flow

Front 19

Describe how the following factors DECREASE the RATE of drug distribution:

- Lipid solubility (Kp)
- Ionization (charge)
- Molecular weight
- Blood flow

Back 19

- ↓ Lipid solubility
- Electrically charged
- ↑ molecular weight
- ↓ Blood flow

Front 20

Define pharmacodynamic

A. drugs react w/ receptor & create a reaction
B. how drug molecules move around the body

Back 20

A. drugs react w/ receptor & create a reaction

Front 21

Define pharmacokinetic

A. drugs react w/ receptor & create a reaction
B. how drug molecules move around the body

Back 21

B. how drug molecules move around the body

(1 drug can displace another drug to create a higher conc. of the displaced drug)

Front 22

T/F
The kidney can filter free, unbound drug molecules.

Back 22

True

Front 23

T/F
There is a barrier b/t CSF & brain and no barrier b/t CSF & blood

Back 23

False

- NO barrier b/t CSF & Brain
- Barrier b/t CSF & Blood

(Blood/Brain barrier)
(Blood/CSF barrier)

Front 24

Match the types of capillaries to the area of the body
- Fenestrations
- Zonula occludens (tight junctions)
- Macular (spot) junctions

A. Capillary Endothelial Cells
B. Kidney
C. Blood Brain Barrier

Back 24

A. Capillary Endothelial Cells = Macular (spot junctions)
B. Kidney = Fenestrations
C. BBB = Zonula occludens (tight junctions)

Front 25

If a free, unbound drug is not filtered by the kidney, how can it be eliminated?

Back 25

Active transport or secretion

Front 26

In the kidney, a highly polar drug is filtered and, once in the tubular fluid, the polar drug can NOT be actively reabsorbed, therefore, it is eliminated.

A. both statements are true
B. both statements are false
C. the 1st statement is true, the 2nd statement is false
D. the 1st statement is false, the 2nd statement is true

Back 26

D. the 1st statement is false, the 2nd statement is true

(NON-polar drugs are filtered)
(Polar drugs cannot be reabsorbed once in tubular fluid)

Front 27

Can drugs cross the placenta?

Back 27

Yes

(as long as they are SMALL and NEUTRAL)

Front 28

A change in the chemical structure of the drug molecule describes ____ of drug metabolism

A. Phase I
B. Phase II
C. Phase III

Back 28

A. Phase I

Front 29

A combination (conjugation) of the drug molecule with a 2nd endogenous substance describes ____ of drug metabolism

A. Phase I
B. Phase II
C. Phase III

Back 29

B. Phase II

Front 30

What is the major enzyme in drug metabolism in the liver?

Back 30

Cytochrome P450

(especially CYP3A)

Front 31

If Cytochrome P450 is INHIBITED while taking 2 different drugs, what potential problem can occur?

Back 31

Potentiation of drug with lower plasma protein biniding affinity
(decreased metabolism)

Can lead to toxicity

Front 32

If Cytochrome P450 is INDUCED while taking 2 different drugs, what potential problem can occur?

Back 32

Decreased effect of the 2nd drug

(increased metabolism)

Front 33

Name 4 Phase I oxidation reactions mediated by Cytochrome P450

Back 33

- Hydroxylation
- Epoxidation
- Reduction
- Dealkylation

(HERD)

Front 34

Name 3 Phase I oxidation reactions NOT mediated by Cytochrome P450

Back 34

- Hydrolytic
- Reduction
- Dehydration (alcohol, aldehyde)

(HRD)

Front 35

Name 5 Phase II Reactions

Back 35

- Glucuronidation
- Acetylation
- Glutathione conjugation
- Amino Acid conjugation
- Sulfate conjugation

(GAGAS)

Front 36

Which of the following determine the rate of clearance of drugs by the kidney?

A. Glomerular filtration
B. Tubular reabsorption
C. Tubular secretion
D. All of the above

Back 36

D. All of the above

Front 37

Which of the following is FALSE?

A. Protein-bound drug molecules will be freely filtered
B. Tubular reabsorption is passive diffusion
C. Tubular secretion involves active transport
D. All statements are true
E. All statements are false

Back 37

A. Protein-bound drug molecules will be freely filtered

(NON-bound drugs are freely filtered)

Front 38

Drugs that are ONLY FILTERED will be cleared at a rate ___ GFR

A. =
B. <
C. >

Back 38

A. =

(CR = 1)

Front 39

Drugs that are FILTERED & REABSORBED will be cleared at a rate ___ GFR

A. =
B. <
C. >

Back 39

B. <

(CR < 1)

Front 40

Drugs that are FILTERED & SECRETED will be cleared at a rate ___ GFR

A. =
B. <
C. >

Back 40

C. >

(CR > 1)

Front 41

T/F
Drugs can be secreted in breast milk.

Back 41

True

Front 42

This process is where non-protein bound drug molecules will be freely filtered

A. Glomerular filtration
B. Tubular reabsorption
C. Tubular secretion

Back 42

A. Glomerular filtration

Front 43

This process involves passive diffusion, depending on concentration, molecular size, Kp, and ionization of a drug.

A. Glomerular filtration
B. Tubular reabsorption
C. Tubular secretion

Back 43

B. Tubular reabsorption

Front 44

This process involves active transport, primarily of anions

A. Glomerular filtration
B. Tubular reabsorption
C. Tubular secretion

Back 44

C. Tubular secretion

Front 45

Drugs that are ONLY FILTERED will be cleared at a rate ___ to the GFR (or CR)

A. =
B. <
C. >

Back 45

A. =

Front 46

Drugs that are FILTERED & REABSORBED will be cleared at a rate ___ to the GFR (or CR)

A. =
B. <
C. >

Back 46

B. <

Front 47

Drugs that are FILTERED & SECRETED will be cleared at a rate ___ to the GFR
(or CR)

A. =
B. <
C. >

Back 47

C. >

Front 48

What is the formula for Clearance Ratio (CR)?

Back 48

CR = Cl / GFR

Front 49

What is the best way to increase elimination of a weak base in the urine?

A. alkalinize with sodium bicarbonate
B. acidify with sodium bicarbonate
C. alkalinize with ammonium chloride
D. acidify with ammonium chloride

Back 49

D. acidify with ammonium chloride

Front 50

Name 5 sites where ion trapping can occur

Back 50

1. urine
2. stomach
3. liver
4. lungs (exhalation)
5. breast milk

(BULLS)

Front 51

Drugs eliminated at a constant AMOUNT per unit time describes:

A. zero order elimination
B. first order elimination
C. second order elimination

Back 51

A. zero order elimination

Front 52

Drugs eliminated at a constant FRACTION per unit time describes:

A. zero order elimination
B. first order elimination
C. second order elimination

Back 52

B. first order elimination

Front 53

What is the formula for half-life (T1/2)?

Back 53

T1/2 = 0.7 / Ke

Front 54

What is the formula for the Elimination Constant (Ke)?

Back 54

Ke = 0.7 / T1/2

Ke = Cl / Vd

Front 55

How many half-lives does it take for 95% of a drug to be eliminated?

Back 55

~4.5 half-lives

Front 56

What is the formula for clearance (Cl)?

Back 56

Cl = (Ke)(Vd)

Front 57

What is the formula for Steady-State Plasma Concentration (Css)?

Back 57

Css = Q / Cl

Css = Q / (Ke)(Vd)

(Q = infusion rate)
(Cl x Css = elimination rate)

Front 58

What is the formula for the Infusion Rate (Q)?

Back 58

Q = Css x Cl

Q = (Css)(Ke)(Vd)

Front 59

How many half-lives does it take to reach a new Css?

Back 59

4.5

Front 60

T/F
The amount of time it takes to reach Css depends on Ke and Q.

Back 60

False

(Depends on Cl only = Ke)

Front 61

What is the formula for Loading Dose (LD)?

Back 61

LD = Css x Vd

Front 62

Give the % body weight of each body compartment

- Total body water
- Extracellular Fluid
- Intracellular Fluid
- Intravascular Fluid (Plasma)
- Interstitial Fluid

Back 62

- Total body water = 60%
- Extracellular Fluid = 20%
- Intracellular Fluid = 40%
- Intravascular Fluid (Plasma) = 4%
- Interstitial Fluid = 16%

Front 63

Host defense mechanism to arrest blood loss from injured blood vessels describes:

A. Hemostasis
B. Thrombosis

Back 63

A. Hemostasis

Front 64

Pathological conditions in which thrombi form and/or occlude blood vessels in organs describes:

A. Hemostasis
B. Thrombosis

Back 64

B. Thrombosis

Front 65

What are the 2 most important cofactors in the Coagulation Cascade?

Back 65

1) TF III
2) Ca²⁺ Phospholipid

Front 66

What 2 roles does thrombin have in blood coagulation?

Back 66

- Converts fibrinogen into FIBRIN
- Activates platelets

Front 67

T/F
Coagulation factors are plasma glycoproteins produced by the spleen in a Vitamin E-dependent way.

Back 67

False

- Produced by HEPATOCYTES (liver)
- VITAMIN K-dependent way

Front 68

VEINS contain ____ thrombi, while ARTERIES contain ____ thrombi.

- Red
- White
- Blue
- No

Back 68

Veins = Red (trapped RBCs)
Arteries = White (No trapped RBCs)

Front 69

Warfarin is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 69

A. Anticoagulant

Front 70

Heparin is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 70

A. Anticoagulant

Front 71

Vitamin K is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 71

A. Anticoagulant

Front 72

Aspirin is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 72

B. Anti-platelet

Front 73

Dipyridamole is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 73

B. Anti-platelet

Front 74

Streptokinase is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 74

C. Thrombolytic drug

Front 75

Tissue Plasminogen Activator (t-PA) is a(n):

A. Anticoagulant
B. Anti-platelet
C. Thrombolytic drug
D. Coagulant

Back 75

C. Thrombolytic drug

Front 76

Heparin & LMWH are taken:

A. orally
B. parenterally

Back 76

B. parenterally

(Heparin = IV infusion)
(LMWH = Sub-Cutaneous)

Front 77

Heparin & LMWH are ____ inhibitors of the coagulation cascade:

A. Direct
B. Indirect

Back 77

B. Indirect

(activates Anti-thrombin III (AT III), which blocks clotting factors)

Front 78

What is the Mechanism of Action of Heparin?

A. Prevents the action of clotting factors by blocking the reduction of Vit KO to Vit KH
B. Acetylates cyclooxygenase, rendering it inactive
C. inhibits cAMP Phosphodiesterase, to prevent the breakdown of intracellular cAMP, thus blocking platelet activation
D. activates Antithrombin (AT III), which neutralizes thrombin & other clotting factors

Back 78

D. activates Antithrombin (AT III), which neutralizes thrombin & other clotting factors

Front 79

What is the Mechanism of Action of Warfarin?

A. Prevents the action of clotting factors by blocking the reduction of Vit KO to Vit KH
B. Acetylates cyclooxygenase, rendering it inactive
C. inhibits cAMP Phosphodiesterase, to prevent the breakdown of intracellular cAMP, thus blocking platelet activation
D. activates Antithrombin (AT III), which neutralizes thrombin & other clotting factors

Back 79

A. Prevents the action of clotting factors by blocking the reduction of Vit KO to Vit KH

Front 80

What is the Mechanism of Action of Aspirin?

A. Prevents the action of clotting factors by blocking the reduction of Vit KO to Vit KH
B. Acetylates cyclooxygenase, rendering it inactive
C. inhibits cAMP Phosphodiesterase, to prevent the breakdown of intracellular cAMP, thus blocking platelet activation
D. activates Antithrombin (AT III), which neutralizes thrombin & other clotting factors

Back 80

B. Acetylates cyclooxygenase, rendering it inactive

Front 81

What is the Mechanism of Action of Dipyridamole?

A. Prevents the action of clotting factors by blocking the reduction of Vit KO to Vit KH
B. Acetylates cyclooxygenase, rendering it inactive
C. inhibits cAMP Phosphodiesterase, to prevent the breakdown of intracellular cAMP, thus blocking platelet activation
D. activates Antithrombin (AT III), which neutralizes thrombin & other clotting factors

Back 81

C. inhibits cAMP Phosphodiesterase, to prevent the breakdown of intracellular cAMP, thus blocking platelet activation

Front 82

T/F
Heparin can cross the placenta, so cannot be used during pregnancy.

Back 82

False

(Does NOT cross placenta, CAN be used during pregnancy)
(Warfarin crosses placenta)

Front 83

T/F
A major advantage of Heparin over LMWH is that it is more predictable, therefore, no monitoring is required.

Back 83

False

LMWH is more predictable

Front 84

T/F
LMWH has a longer half-life than Heparin

Back 84

True

Front 85

What are 2 major complications of heparin?

Back 85

1) hemorrhage
2) Heparin Induced Thrombocytopenia (HIT)

Front 86

Warfarin is taken:

A. orally
B. parenterally

Back 86

A. Orally

Front 87

In plasma, 99% of warfarin is bound to albumin. Only the bound form is active.


A. both statements are true
B. both statements are false
C. the 1st statement is true, the 2nd statement is false
D. the 1st statement is false, the 2nd statement is true

Back 87

C. the 1st statement is true, the 2nd statement is false

(only the FREE FORM is active)

Front 88

T/F
Warfarin can cross the placenta, so cannot be used during pregnancy.

Back 88

True

Front 89

What is the action of plasmin?

A. attracts platelets
B. converts fibrinogen to fibrin
C. degrades fibrin
D. prevents platelet formation

Back 89

C. degrades fibrin

Front 90

Tissue Plasminogen Activator (t-PA) is synthesized by:

A. endothelial cells
B. epithelial cells
C. hepatocytes
D. kidney

Back 90

A. endothelial cells

Front 91

tPA is a ____ protease

A. serine
B. glycine
C. proline
D. lysine

Back 91

A. serine

Front 92

In plasma, urokinase exists as a _____

A. non-bound molecule
B. zymogen
C. active compound
D. lysine protease

Back 92

B. zymogen

Front 93

Urokinase is synthesized by:

A. endothelial cells
B. epithelial cells
C. hepatocytes
D. kidney

Back 93

D. kidney

Front 94

T/F
Streptokinase is fibrin-specific.

Back 94

False

(It is NOT fibrin specific, leading to degradation of fibrinogen & fibrin)

Front 95

What are the 4 main ways to prevent platelet formation?

Back 95

1) COX inhibitor
2) block ADP receptor (P2Y12)
3) ↑ cAMP
4) Block platelet receptors (GPIIb-IIIa)

Front 96

Dipyridamole is used in combination with _____ to prevent thromboembolism in patients w/ artificial heart valves.

A. Aspirin
B. Clopidogrel
C. Heparin
D. Warfarin

Back 96

D. warfarin

Front 97

What are the 2 main functions of signal-transducing receptors?

Back 97

1) sensing ligand
2) transmitting message

Front 98

These drug receptors include enzymes, transporters, channels, structural proteins, and nucleic acids. They also require no ligand to create an effect.

A. Non-receptor mediated
B. Signal-transducing

Back 98

A. Non-receptor mediated

Front 99

These drug receptors include the use of hormones, neurotransmitters, autacoids, growth factors, and cytokines.

A. Non-receptor mediated
B. Signal-transducing

Back 99

B. Signal-transducing

Front 100

A cummulative percentage of subjects exhibiting a defined effect for both toxic & therapeutic effects describes:

A. Quantal (All-or-None) Response
B. Graded (Dose) Response

Back 100

A. Quantal (All-or-None) Response

Front 101

A response to a drug that is described as a percentage of the maximal response is:

A. Quantal (All-or-None) Response
B. Graded (Dose) Response

Back 101

B. Graded (Dose) Response

Front 102

The magnitude of effect is proportional to the concentration of the drug-receptor complex [RD] describes:

A. Fractional occupancy
B. Quantal response
C. Occupational theory
D. Modified Occupational theory

Back 102

C. Occupational Theory

Front 103

A maximum effect produced when an agonist occupies only a fraction of the receptors. Therefore, the response is NOT linearly proportional to the number of receptors occupied.

A. Fractional occupancy
B. Quantal response
C. Occupational theory
D. Modified Occupational theory

Back 103

D. Modified Occupational theory

Front 104

What is the formula for the Equilibrium Dissociation Constant (Kd)?

Back 104

Kd = K₂/K₁ = [R][D] / [RD]

Front 105

1) What is the formula for Effect?

2) Which theory does it belong to, Occupational or Modified Occupational?

Back 105

Effect = (Max. Effect) [D] / (Kd +[D])

Occupational Theory

Front 106

__ represents the affinity of the drug to its receptor

A. Kd
B. k₁
C. k₂
D. k₃

Back 106

A. Kd

Front 107

___ is usually limited by the rates of diffusion of the molecule, therefore, has little to do with affinity.


A. Kd
B. k₁
C. k₂
D. k₃

Back 107

B. k₁

Front 108

Kd is dependent on ___

A. k₁
B. k₂
C. k₃

Back 108

B. k₂

Front 109

Low Kd = ___ affinity = ___ to dissociate

A. high, difficult
B. high, easy
C. low, difficult
D. low, easy

Back 109

A. high, difficult

Front 110

High Kd = ___ affinity = ___ to dissociate

A. high, difficult
B. high, easy
C. low, difficult
D. low, easy

Back 110

D. low, easy

Front 111

When do you have 1/2 max binding of a ligand to a receptor

Back 111

When Kd = [D]

Front 112

A linear concentration scale of a Graded (Dose) Response curve yields a:

A. sigmoidal curve
B. rectangular hyperbolic curve

Back 112

B. rectangular hyperbolic curve

Front 113

A logarithm of concentration scale of a Graded (Dose) Response curve yields a:

A. sigmoidal curve
B. rectangular hyperbolic curve

Back 113

A. sigmoidal curve

Front 114

What is related to the dosage of a drug required to produce given effect?

A. Potency
B. Efficacy

Back 114

A. potency

Front 115

What is the magnitude of effect that can be produced by a drug?

A. Potency
B. Efficacy

Back 115

B. Efficacy

Front 116

If you are increasing the concentration of a drug to get the same effect, then you have a(n) ___ potency.

A. lower
B. higher
C. equal

Back 116

A. lower

Front 117

Which of the following is NOT possible for 2 drugs:

A. Same potency, same efficacy
B. Different potency, different efficacy
C. Same potency, different efficacy
D. Different potency, same efficacy
E. All of the above are possible
F. None of the above are possible

Back 117

E. All of the above are possible

Front 118

A drug that interacts w/ a receptor and produces effects by "activating" the receptor:

A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 118

A. Agonist

Front 119

Reversibly competes at binding sites, and can be overcome by increasing the concentration of agonist

A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 119

B. competitive antagonist

Front 120

Irreversibly interacts at binding sites. Equivalent to removing receptors from the system.

A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 120

C. Non-Competitive antagonist

Front 121

Has intermediate efficacy of full agonist and antagonist. Their responses are dependent on tissue or specific effect.

A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 121

D. Partial Agonist

Front 122

Potencies vary independently of efficacy


A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 122

D. Partial Agonist

Front 123

A compound that has higher affinity for the inactive receptor (Ri) than the active receptor (Ra)

A. Agonist
B. Competitive antagonist
C. Non-Competitive antagonist
D. Partial Agonist
E. Inverse Agonist

Back 123

E. Inverse Agonist

Front 124

__ can be taken as a measure of efficacy.

A. Kd
B. k₁
C. k₂
D. k₃

Back 124

D. k₃

Front 125

_____ have zero efficacy

A. Agonist
B. Antagonist
C. Partial Agonist
D. Inverse Agonist

Back 125

B. antagonist

Front 126

Name 4 ways receptors are identified

Back 126

1) Structure
2) Binding of radioactive ligand (labeling)
3) Molecular cloning
4) Genome project

Front 127

Adrenergic & muscarinic cholinergic receptors are examples of:

A. G-protein-coupled receptors
B. Ligand-regulated ion channels
C. Tyrosine Kinase-linked receptors
D. Guanyl cyclase-linked receptors
E. Cytosolic/Nuclear receptors

Back 127

A. G-protein-coupled receptors

Front 128

Describe G-protein-coupled receptor mechanism of action

Back 128

1) ligand binds (GDP bound at rest)
2) α releases GDP (binds GTP)
3) βγ subunit activates/inhibits effectors
4) α hydrolyzes GTP & becomes inactive
5) βγ subunits re-unite with α-GDP to form inactive G-protein

Front 129

What are the 3 main subunits of Gα?

Back 129

1) Gs
2) Gi
3) Gq

Front 130

What is the main function of Gs?

I. Stimulate
II. Inhibit
III. Adenylyl cyclase
IV. Phospholipase C

A. I & III
B. I & IV
C. II & III
D. II & IV

Back 130

A. I & III
= stimulates adenylyl cyclase

(↑ cAMP, activates Protein Kinase A)

Front 131

What is the main function of Gi?

I. Stimulate
II. Inhibit
III. Adenylyl cyclase
IV. Phospholipase C

A. I & III
B. I & IV
C. II & III
D. II & IV

Back 131

C. II & III
= inhibits adenylyl cyclase

(↓ cAMP formation)
(also K⁺ & Ca²⁺ channels)

Front 132

What is the main function of Gq?

I. Stimulate
II. Inhibit
III. Adenylyl cyclase
IV. Phospholipase C

A. I & III
B. I & IV
C. II & III
D. II & IV

Back 132

B. I & IV
= stimulates phospholipase C

(↑ IP3 & DAG)

Front 133

Nicotinic cholinergic receptors, GABA, glycine, & glutamate receptors are examples of:

A. G-protein-coupled receptors
B. Ligand-regulated ion channels
C. Tyrosine Kinase-linked receptors
D. Guanyl cyclase-linked receptors
E. Cytosolic/Nuclear receptors

Back 133

B. Ligand-regulated ion channels

Front 134

Ligand-regulated ion channels use membrane depolarization to transmit signals _____

A. quickly
B. slowly

Back 134

A. quickly

Front 135

Growth factors, such as EGF, PDGF, NGF, and insulin use:

A. G-protein-coupled receptors
B. Ligand-regulated ion channels
C. Tyrosine Kinase-linked receptors
D. Guanyl cyclase-linked receptors
E. Cytosolic/Nuclear receptors

Back 135

C. Tyrosine kinase-linked receptors

Front 136

T/F
Kinase activity usually dephosphorylates the receptor, activating it, so it may interact with other signaling molecules.

Back 136

False

(it PHOSPHORYLATES the receptor)

Front 137

T/F
Tyrosine kinase-linked receptors are faster than Ligand-regulated ion channels

Back 137

False

(Tyrosine kinase-linked receptors are SLOW)
↓
(Involved in cell growth/death)

Front 138

____ are receptors for NO

A. G-protein-coupled receptors
B. Ligand-regulated ion channels
C. Tyrosine Kinase-linked receptors
D. Guanyl cyclase-linked receptors
E. Cytosolic/Nuclear receptors

Back 138

D. Guanyl cyclase-linked receptors

Front 139

Receptors for steroids and thyroid hormone


A. G-protein-coupled receptors
B. Ligand-regulated ion channels
C. Tyrosine Kinase-linked receptors
D. Guanyl cyclase-linked receptors
E. Cytosolic/Nuclear receptors

Back 139

E. Cytosolic/Nuclear receptors

Front 140

Match the Drug to it's Mechanism of action

- Abciximab (ReoPro)
- Aspirin
- Clopidogrel
- Dipyridamole

A. ADP receptor (P2Y12) antagonist
B. Increases cAMP
C. COX inhibitor
D. GPIIb-IIIa (fibrinogen receptor) antagonist

Back 140

A. ADP receptor (P2Y12) antagonist = Clopidogrel
B. Increases cAMP = Dipyridamole
C. COX inhibitor = Aspirin
D. GPIIb-IIIa (fibrinogen receptor) antagonist = Abciximab (ReoPro)