U2.1 DRG PHARMACODYNAMICS & RECEPTORS

Question 1

Actions or effects of the drug on the body

Answer 1

Pharmacodynamics

Question 2

plays a major role in deciding whether a group is appropriate therapy for a particular symptom or disease

Answer 2

Pharmacodynamics

Question 3

Specific molecules/target molecules of the drug so that they could interact with the body that produce changes in the function of the system

Answer 3

Receptors

Question 4

Determine the quantitative relations between dose or concentration of drug and pharmacologic effects

Answer 4

Receptors

Question 5

measurable to its pharmacologic effects

Answer 5

Dose

Question 6

Drugs are _______ in choosing a drug molecule to bind to avoid constant activation or inhibition by promiscuous binding of many different molecules

Answer 6

Selective

Question 7

Drugs have _______ binding and _________ with receptors

Answer 7

Selective binding and specificity

Question 8

Changes its function upon binding in such a way that the function of the biologic system is altered in order to have pharmacologic effect

Answer 8

Receptors

Question 9

Receptors are ___________ in ligand binding characteristics (respond to proper chemical signals and not to meaningless ones)

Answer 9

selective

Question 10

Mediate the actions of both pharmacologic agonists and antagonists

Answer 10

Receptors

Question 11

Most receptors are ______ which provide the necessary diversity and specificity of shape and electrical charge

Answer 11

proteins

Question 12

Specific binding region of the macromolecule

Answer 12

Receptor Site or Recognition Site

Question 13

happens to the drug when there is an interaction between the drug and the receptor

Answer 13

initiates the action of the drug

Question 14

Receptor sites have _______ and _______ affinity to the drug molecule.

Answer 14

High and selective affinity

Question 15

T/F Even if the drug enters the body, but it cannot reach the target receptor, it will still take effect

Answer 15

F; it will not take effect

Question 16

Classification of Receptors

Best characterized drug receptors

Answer 16

Regulatory Proteins

Question 17

Classification of Receptors

Mediates the action of endogenous chemical signals like neurotransmitters, autacoids, and hormones

Answer 17

Regulatory Proteins

Question 18

Classification of Receptors

Mediates the effects of the most useful therapeutic agents as it takes effect immediately

Answer 18

Regulatory Proteins

Question 19

Classification of Receptors

Inhibited (or less commonly, activated) by binding a drug

Answer 19

Enzymes

Question 20

Classification of Receptors

Na+/K+ ATPase Pump, the membrane
receptor for digitalis

Answer 20

Transport Proteins

Question 21

Classification of Receptors

Stabilizes Tubulin

Answer 21

Structural Proteins

Question 22

Molecules that translate the drug-receptor interaction into a change in cellular activity

Answer 22

Effectors

Question 23

T/F Some receptors are also effectors

Answer 23

True

Question 24

Signaling Mechanism

________ drug that crosses the plasma membrane and acts on intracellular receptors

Answer 24

Lipid-soluble

Question 24

T/F A single molecule may incorporate both the drug binding site and the effector mechanism

Answer 24

True

Question 25

Signaling Mechanism Steroids

Answer 25

Lipid-soluble drugs

Question 26

Signaling Mechanism Where steroid attaches to alter genetic transcription

Answer 26

hsp90

Question 27

Signaling Mechanism Transmembrane receptor protein-intracellular enzymatic activity is regulated by a _________ that binds to the proteins’ extracellular domain

Answer 27

ligand

Question 28

Signaling Mechanism Transmembrane Receptors that binds and stimulates a ____________

Answer 28

Tyrosine kinase

Question 29

Signaling Mechanism Other term for Protein Tyrosine Kinase Associated receptors

Answer 29

JAK - Janus Kinase

Question 30

Signaling Mechanism Type of receptor that causes dimerization

Answer 30

Transmembrane receptors that stimulates protein tyrosine kinase

Question 31

Signaling Mechanism Insulin

Answer 31

Transmembrane receptors that bind and stimulates protein tyrosine kinase

Question 32

Signaling Mechanism _______________ transmembrane ion channel: which regulates the opening of the ion channel

Answer 32

Ligand-gated

Question 33

Signaling Mechanism causes drug to mimic or block the action of agonists

Answer 33

ligand-gated ion channels

Question 34

Signaling Mechanism Type of receptor that is similar to our neurotransmitter receptors

Answer 34

Ligand-gated transmembrane ion channel

Question 35

Signaling Mechanism GABA, excitatory acetylcholine

Answer 35

ligand-gated transmembrane ion channel

Question 36

Signaling Mechanism Receptors transmit its signal across the plasma membrane by (increasing/decreasing) transmembrane conductance of the relevant ion

Answer 36

Increasing transmembrane conductance

Question 37

Signaling Mechanism Binding site of Acetylcholine outside to allow opening of a central aqueous transmembrane ion channel where sodium enters

Answer 37

α biding sites

Question 38

Signaling Mechanism Catecholamine / epinephrine

Answer 38

Transmembrane receptor coupled with G protein

Question 39

Signaling mechanism Increasing the intracellular concentrations of second messengers

Answer 39

Transmembrane receptor coupled with G protein

Question 40

modulate the production of intracellular messengers

Answer 40

G protein

Question 41

Type of G protein ↑ Adenylyl cyclase → ↑ cAMP

Answer 41

Gs, Golf

Question 42

Type of G protein Receptor for - β-Adrenergic amines - Histamine - Serotonin - Glucagon - Many other hormones

Answer 42

Gs

Question 43

Type of G protein ↓ Adenylyl cyclase → ↓ cAMP

Answer 43

Gi1, Gi2, Gi3

Question 44

Type of G protein Open cardiac K+ channels → ↓ heart rate

Answer 44

Gi1, Gi2, Gi3

Question 45

Type of G protein receptor for - α2-Adrenergic amines - Acetylcholine (muscarinic) - Opioids Serotonin - Many others

Answer 45

Gi1, Gi2, Gi3

Question 46

Type of G protein Receptor for Odorants (olfactory epithelium)

Answer 46

Golf

Question 47

Type of G protein Receptors for Neurotransmitters in brain (not yet specifically identified)

Answer 47

Go

Question 48

Type of G protein ↑ Phospholipase C → ↑ IP3, diacylglycerol, cytoplasmic Ca2+

Answer 48

Gq

Question 49

Type of G protein Receptors for - Acetylcholine (muscarinic) - Bombesin - Serotonin (5-HT2) - Many others

Answer 49

Gq

Question 50

Type of G protein Receptors for Photons (rhodopsin and color opsins in retinal rod and cone cells)

Answer 50

Gt1, Gt2

Question 51

Type of G protein ↑ cGMP phosphodiesterase → ↓ cGMP (phototransduction)

Answer 51

Gt1, Gt2

Question 52

Intracellular Second Messengers Mediates hormonal responses

Answer 52

cAMP (Cyclic adenosine monophosphate)

Question 53

Intracellular Second Messengers cAMP mobilizes stored energy (breakdown of carbohydrates in the liver stimulated by _____________

Answer 53

catecholamines

Question 54

cAMP Conservation of water by the kidneys mediated by ___________

Answer 54

vasopressin

Question 55

cAMP Calcium homeostasis

Answer 55

Parathyroid hormone

Question 56

cAMP Heart rate and contraction by

Answer 56

beta-adrenomimetic catecholamines

Question 57

T/F cAMP is a product of the enzyme adenylyl cyclase and it converts ATP to cAMP

Answer 57

T

Question 58

stop the effect of your cAMP

Answer 58

Phosphatase

Question 59

Intracellular Second Messengers Bind to receptors linked to G proteins while other bind to receptor tyrosine kinases

Answer 59

Calcium and Phosphoinositides

Question 60

Intracellular Second Messengers Calcium and Phosphoinositides stimulates the membrane enzyme __________

Answer 60

phospholipase C

Question 61

Intracellular Second Messengers phospholipase C cleaves PIP2 into

Answer 61

diacylglycerol (DAG) and Inositol Triphosphate (IP3)

Question 62

Calcium and Phosphoinositides release the Calcium (Ca2+)

Answer 62

Inositol Triphosphate (IP3)

Question 63

Intracellular Second Messengers Few signaling roles in a few cell types like the intestinal mucosa and vascular smooth muscle cells

Answer 63

cGMP (Cyclic guanosine monophosphate)

Question 64

Intracellular Second Messengers Causes Relaxation of vascular smooth muscles by a kinase-mediated mechanism

Answer 64

cGMP (Cyclic guanosine monophosphate)