Exam 1

Question 1

Agonist

Answer 1

Activate receptor and cause a favorable conformational change that activates a second messenger cascade

Question 2

Antagonist

Answer 2

Minimal conformational change causes no second messenger cascade, no activation of receptor, prevents agonist interaction

Question 3

Inverse agonist

Answer 3

Causes alternate conformational change and a different second messenger cascade can happen or it turns the receptor off

Question 4

M1

Answer 4

parietal cells

Question 5

M2

Answer 5

Nerve terminals

Question 6

M3

Answer 6

smooth muscle

Question 7

Nn

Answer 7

post-ganglionic cell body

Question 8

Nm

Answer 8

skeletal muscle cells

Question 9

Full agonist

Answer 9

maximal effect

Question 10

Partial agonist

Answer 10

low efficacy,
reduced maximal effect,
tickles receptor,
can act as antagonist for full agonist

Question 11

Antagonist efficacy

Answer 11

Competitive
No efficacy (effect)

Question 12

Competitive antagonists

Answer 12

Bind reversibly to the receptor
Can be overcome if increase concentration of agonist
Will not alter the maximal effect of an agonist
Most common antagonist
Dynamic (binds and releases)
Increase antagonist –> decrease apparent potency

Question 13

Irreversible antagonist

Answer 13

Bind to the receptor in an irreversible manner
Will reduce the maximal effect of an agonist
Rare
Static
Increase irreversible –> decrease max response, and decrease apparent potency

Question 14

Noncompetitive antagonists

Answer 14

Bind to a site adjacent to the receptor (decrease ability of receptor to be activated by agonist)
Interfere with receptor-effector coupling mechanisms (change binding site)
Have similar effect on the agonist concentration response curve as an irreversible antagonist but is reversible

Question 15

Cellular response to an agonist

Answer 15

1. A direct intercellular effect

2. Activation of an amplifying second messenger cascade

Question 16

Drug Tolerance

Answer 16

1. Receptor desensitization
2. Tolerance (require higher doses to get same response)
3. Resistance

Question 17

Additive effect

Answer 17

The effect of two drugs is equal to the sum of their individual effects

Question 18

Synergistic effect

Answer 18

The effect of two drugs i greater than the sum of their individual effects

Question 19

Potentiation

Answer 19

A drug which alone has no effect enhances the potency of a drug which does have an effect

Question 20

Receptor antagonism

Answer 20

A drug with no effect inhibits effect of another drug

Question 21

Functional antagonism

Answer 21

Effect of one agonist opposes the effect of another agonist

Question 22

Median effective dose

Answer 22

Dose of drug at which 50% of individuals demonstrate the desired therapeutic effect

Question 23

Median lethal dose

Answer 23

Dose of drug causing death in 50% of subjects

Question 24

Cytarebine (Ara-C)

Answer 24

Causes DNA damage, Cancer

Question 25

Yondelis (Trabectedin)

Answer 25

Causes DNA backbone cleavage, Cancer

Question 26

Prialt (Ziconotide)

Answer 26

Selective Blocker, Pain

Question 27

Vidarabine (Ara-A)

Answer 27

Blocks viral DNA synthesis, antiviral agent

Question 28

Eribulin

Answer 28

Blocks microtubule formation, Cancer

Question 29

Bryostatin 1

Answer 29

Modulates PKC activity, failed clinical trials

Question 30

Salinosporamide A (Marizomib)

Answer 30

Irreversibly inhibits the proteosome, Cancer

Question 31

Pacleteaxel (Taxol)

Answer 31

Stabilizes microtubule dynamics, Cancer